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BI-78D3

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BI-78D3  纯度: 99.49%

BI-78D3 是一种底物竞争性的 JNK 抑制剂，抑制 JNK 激酶活性，IC50 为 280 nM。

BI-78D3

BI-78D3 Chemical Structure

CAS No. : 883065-90-5

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥968 In-stock
5 mg ￥880 In-stock
10 mg ￥1350 In-stock
25 mg ￥2850 In-stock
50 mg ￥4950 In-stock
100 mg ￥8100 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

BI-78D3 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • MAPK Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Diabetes Related Compound Library
  • Oxygen Sensing Compound Library
  • Anti-Parkinson’s Disease Compound Library
  • Anti-Obesity Compound Library
  • Transcription Factor Targeted Library
  • Targeted Diversity Library

生物活性

BI-78D3 functions as a substrate competitive inhibitor of JNK, inhibit the JNK kinase activity (IC50=280 nM).

IC50 & Target[1]

JNK

280 nM (IC50)

体外研究
(In Vitro)

BI-78D3, dose-dependently inhibits the phosphorylation of JNK substrates both in vitro and in cell. BI-78D3 is able to compete with the D-domain of JIP1 (amino acids 153-163; pepJIP1) for JNK1 binding (IC50=500 nM). Using the same in vitro LanthaScreen kinase assay and the same ATF2 substrate, BI-78D3 is found to be 100-fold less active vs. p38α, a member of the MAPK family with high structural similarity to JNK, and completely inactive against mTOR and PI3-kinase (α-isoform), both unrelated protein kinases. Furthermore, Lineweaver-Burk analysis clearly indicates that BI-78D3 is competitive with ATF2 for binding to JNK1 with an apparent Ki value of 200 nM. In an attempt to profile the properties of BI-78D3 in the context of a complex cellular milieu, the cell-based LanthaScreen kinase assay is used. In this assay BI-78D3 is able to inhibit TNF-α stimulated phosphorylation of c-Jun in cell (EC50=12.4 μM)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

The link between ConA-induced liver failure, TNF receptor signaling, and JNK function has been established by studies employing JNK1-/- and JNK2-/- mice. For this analysis, insulin insensitive mice are injected only once with 25 mg/kg BI-78D3, 30 min before insulin injection. The effect of insulin on blood glucose levels is then measured. BI-78D3 results in a statistically significant reduction in blood glucose levels as compared with the vehicle control. Thus, the ability of BI-78D3 to abrogate ConA-induced liver damage and restore insulin sensitivity is consistent with its proposed function as an effective JNK inhibitor. Liquid chromatography/mass spectrometry bio-availability analysis demonstrates that BI-78D3 has favorable microsome and plasma stability (T1/2=54 min)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

379.37

Formula

C13H9N5O5S2
CAS 号

883065-90-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (263.59 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6359 mL 13.1797 mL 26.3595 mL
5 mM 0.5272 mL 2.6359 mL 5.2719 mL
10 mM 0.2636 mL 1.3180 mL 2.6359 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.59 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.59 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Stebbins JL et al. Identification of a new JNK inhibitor targeting the JNK-JIP interaction site. Proc Natl Acad Sci U S A, 2008 Oct 28, 105(43):16809-13.
Kinase Assay
[1]

The cell based kinase assays for c-Jun and ATF2 phosphorylation carry out by using the LanthaScreen c-Jun (1-79) HeLa and LanthaScreen ATF2 (19-106) A549 cell lines which stably express GFP-c-Jun 1-79 and GFP-ATF2 19-106, respectively. Phosphorylation is determined by measuring the time resolved FRET (TR-FRET) between a terbium labeled phospho-specific antibody and the GFP-fusion protein. The cells are plated in white tissue culture treated 384 well plates at a density of 10,000 cell per well in 32 μl assay medium (supplemented with 1% charcoal/dextran-treated FBS, 100 U/mL Penicillin and 100 μg/mL Streptomycin, 0.1 mM nonessential amino acids, 1 mM sodium pyruvate, 25 mM Hepes, pH 7.3, and lacking phenol red). After overnight incubation, cells are pretreated for 60 min with BI-78D3 (0.001, 0.01, 0.1, 1, 10, and 100 μM) followed by 30 min of stimulation with 2 ng/mL of TNF-α that stimulates both JNK and p38. The medium is then removed by aspiration and the cells are lysed by adding 20 μL of lysis buffer (20 mM Tris•HCl, pH 7.6, 5 mM EDTA, 1% Nonidet P-40 substitute, 5 mM NaF, 150 mM NaCl, and 1:100 protease and phosphatase inhibitor mix, SIGMA P8340 and P2850, respectively). The lysis buffer includs 2 nM of the terbium-labeled anti-pc-Jun (pSer73) or anti-pATF2 (pThr71) detection antibodies. After allowing the assay to equilibrate for 1 h at room temperature, TR-FRET emission ratios are determined on a BMG Pherastar fluorescence plate reader (excitation at 340 nm, emission 520 nm and 490 nm; 100 μs lag time, 200 μs integration time, emission ratio=Em520/Em 490)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Mice[1]
ConA and BI-78D3 is injected i.v. at 10 mg/kg into 6 to 8 weeks old male BL/6 mice. For partial hepatectomy, mice are anesthetized with isofluorane and subjected to midventral laparotomy followed by removal of the left lateral and median lobes. Animals are killed, blood is collected by cardiac puncture, and livers are surgically removed. Serum is separated and analyzed for alanine-aminotranferase levels[1].
Eleven-week-old male BKS.Cg-+Leprdb/+Leprdb/OlaHsd db/db mice are randomized based on blood glucose levels acclimated three days before drug dosing. Blood glucose is read by using a hand-held glucose meter (Mice are fasted 6 h before i.p. (i.p.) administration of 25 mg/kg BI-78D3. Thirty minutes after test article administration, Bovine Insulin (I-0516 at 0.75 mg/kg) is administered via i.p. injection. Blood samples are taken at designated time points and blood glucose levels are measured as described. Food is returned three hours after test article administration[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Stebbins JL et al. Identification of a new JNK inhibitor targeting the JNK-JIP interaction site. Proc Natl Acad Sci U S A, 2008 Oct 28, 105(43):16809-13.

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BI8626

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BI8626  纯度: 95.16%

BI8626 是一种泛素连接酶 HUWE1 特异性拮抗剂，IC50 为 0.9 μM。

BI8626

BI8626 Chemical Structure

CAS No. : 1875036-75-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2750 In-stock
5 mg ￥2500 In-stock
10 mg ￥3800 In-stock
25 mg ￥7000 In-stock
50 mg ￥12500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

BI8626 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Oxygen Sensing Compound Library
  • Ubiquitination Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library

生物活性

BI8626 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 0.9 μM[1].

IC50 & Target

IC50: 0.9 μM (HUWE1)[1]
体外研究
(In Vitro)

BI8626 induces HUWE1 ectopically expresses to abolishe ubiquitination of MCL1 in HeLa cells[1].
BI8626 suppresses colony formation of Ls174T cells with estimated IC50 value of 0.7 μM, and BI8622 (1-4 days) treatment retards passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1[1].
BI8626 (0-50 μM; 0-6 hours) retards the degradation of MCL1 in response to UV irradiation to the same extent as depletion of HUWE1 in U2OS cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: Ls174T cells
Concentration: 0 μM, 5 μM,10 μM, 15 μM, 20 μM
Incubation Time: 0-4 days
Result: Retarded passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1.

Western Blot Analysis[1]

Cell Line: U2OS cells
Concentration: 0 μM, 20 μM, 50 μM
Incubation Time: 0 hour,1 hour,2 hours,4 hours,6 hours
Result: Retarded the degradation of MCL1 in response to UV irradiation in HeLa cells by inhibiting HUWE1 in U2OS cells.

分子量

440.54

Formula

C25H28N8
CAS 号

1875036-75-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL (189.15 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2699 mL 11.3497 mL 22.6994 mL
5 mM 0.4540 mL 2.2699 mL 4.5399 mL
10 mM 0.2270 mL 1.1350 mL 2.2699 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.72 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.72 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Peter S, et al. Tumor cell-specific inhibition of MYC function using small molecule inhibitors of the HUWE1 ubiquitin ligase.EMBO Mol Med. 2014 Dec;6(12):1525-41.

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生物活性分子抑制剂BI-7273

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BI-7273  纯度: 99.83%

BI-7273 是一种选择性的，细胞透过的 BRD9 抑制剂，IC50 和 Kd 分别为 19 和 0.75 nM；同时对 BRD7 的作用较强，IC50 和 Kd 值分别为 117 nM 和 0.3 nM。

BI-7273

BI-7273 Chemical Structure

CAS No. : 1883429-21-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1210 In-stock
5 mg ￥1100 In-stock
10 mg ￥1900 In-stock
25 mg ￥3800 In-stock
50 mg ￥6000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

BI-7273 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.

IC50 & Target

IC50: 19 nM (BRD9), 117 nM (BRD7)[1]
Kd: 0.75 nM (BRD9), 0.3 nM (BRD7)[1]
体外研究
(In Vitro)

BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM. BI-7273 also has slight activity against a panel of kinases such as CECR2, BRPF1, BRD1, CREBBP, EP300, FALZ, TAF1(2) and TAF1L(2), with Kds of 8.8 nM, 210 nM, 2600 nM, 8600 nM, 10000 nM, 850 nM, 1000 nM, and 1200 nM, respectively. BI-7273 (1 μM) is active in U2OS cell lines. BI-7273 blocks EOL-1 cell proliferation with EC50 of 1400 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

353.41

Formula

C20H23N3O3
CAS 号

1883429-21-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 10 mg/mL (28.30 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8296 mL 14.1479 mL 28.2957 mL
5 mM 0.5659 mL 2.8296 mL 5.6591 mL
10 mM 0.2830 mL 1.4148 mL 2.8296 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (2.83 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.83 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 1 mg/mL (2.83 mM); Suspended solution; Need ultrasonic

    此方案可获得 1 mg/mL (2.83 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (2.83 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Martin LJ, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26;59(10):4462-75.
Kinase Assay
[1]

His-tagged BRD9 is immobilized to a density of 2000-4000 RUs on flow cells 3 and 4 of a Biacore NTA-chip. Carbonic anhydrase II is immobilized at a similar density on flow cell 2 and a blank reference surface is generated on flow cell 1. The buffer is then switched to assay buffer (HBS-P+ = 10 mM HEPES, pH 7.4, 150 mM NaCl, 0.05 % P20 + 5 % DMSO) and the chip equilibrated for several hours before use for Kd determinations. To be able to correct for differences in bulk solvent refractive index caused by small variations in the DMSO concentration solvent correction samples are included at the beginning and end of the run. Compounds (BI-7273, etc.) are injected in concentration series (1:1 dilutions, 7 different concentrations), starting with a maximum concentration that is approximately 10-20-fold higher than the expected Kd. The concentration series are prepared in 96-well plates. In the case that the dilution window chosen for a particular compound does not appropriately bracket the Kd of the compound the measurement is repeated with an optimized starting concentration. Positive and negative control samples are included at regular intervals to be able to monitor the performance of the assay. CBS is used as a positive control for carbonic anhydrase II to check for integrity of the reference protein at regular intervals. To correct for the excluded volume effect a DMSO calibration series is prepared and the calibration samples are measured at the beginning and end of each run. Kd values are determined and averaged[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Cells are grown in 50 µL medium for 7 days starting with 500 and with 1000 cells per well of a 384 well plate in the presence of varying concentrations of compound (BI-7273, etc.) before measuring viability via cellular ATP levels using the cell titer glow assay[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Martin LJ, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26;59(10):4462-75.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

生物活性分子抑制剂BI-7273

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
BI-7273  纯度: 99.83%

BI-7273 是一种选择性的，细胞透过的 BRD9 抑制剂，IC50 和 Kd 分别为 19 和 0.75 nM；同时对 BRD7 的作用较强，IC50 和 Kd 值分别为 117 nM 和 0.3 nM。

BI-7273

BI-7273 Chemical Structure

CAS No. : 1883429-21-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1210 In-stock
5 mg ￥1100 In-stock
10 mg ￥1900 In-stock
25 mg ￥3800 In-stock
50 mg ￥6000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

BI-7273 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.

IC50 & Target

IC50: 19 nM (BRD9), 117 nM (BRD7)[1]
Kd: 0.75 nM (BRD9), 0.3 nM (BRD7)[1]
体外研究
(In Vitro)

BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM. BI-7273 also has slight activity against a panel of kinases such as CECR2, BRPF1, BRD1, CREBBP, EP300, FALZ, TAF1(2) and TAF1L(2), with Kds of 8.8 nM, 210 nM, 2600 nM, 8600 nM, 10000 nM, 850 nM, 1000 nM, and 1200 nM, respectively. BI-7273 (1 μM) is active in U2OS cell lines. BI-7273 blocks EOL-1 cell proliferation with EC50 of 1400 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

353.41

Formula

C20H23N3O3
CAS 号

1883429-21-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 10 mg/mL (28.30 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8296 mL 14.1479 mL 28.2957 mL
5 mM 0.5659 mL 2.8296 mL 5.6591 mL
10 mM 0.2830 mL 1.4148 mL 2.8296 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (2.83 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.83 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 1 mg/mL (2.83 mM); Suspended solution; Need ultrasonic

    此方案可获得 1 mg/mL (2.83 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (2.83 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Martin LJ, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26;59(10):4462-75.
Kinase Assay
[1]

His-tagged BRD9 is immobilized to a density of 2000-4000 RUs on flow cells 3 and 4 of a Biacore NTA-chip. Carbonic anhydrase II is immobilized at a similar density on flow cell 2 and a blank reference surface is generated on flow cell 1. The buffer is then switched to assay buffer (HBS-P+ = 10 mM HEPES, pH 7.4, 150 mM NaCl, 0.05 % P20 + 5 % DMSO) and the chip equilibrated for several hours before use for Kd determinations. To be able to correct for differences in bulk solvent refractive index caused by small variations in the DMSO concentration solvent correction samples are included at the beginning and end of the run. Compounds (BI-7273, etc.) are injected in concentration series (1:1 dilutions, 7 different concentrations), starting with a maximum concentration that is approximately 10-20-fold higher than the expected Kd. The concentration series are prepared in 96-well plates. In the case that the dilution window chosen for a particular compound does not appropriately bracket the Kd of the compound the measurement is repeated with an optimized starting concentration. Positive and negative control samples are included at regular intervals to be able to monitor the performance of the assay. CBS is used as a positive control for carbonic anhydrase II to check for integrity of the reference protein at regular intervals. To correct for the excluded volume effect a DMSO calibration series is prepared and the calibration samples are measured at the beginning and end of each run. Kd values are determined and averaged[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Cells are grown in 50 µL medium for 7 days starting with 500 and with 1000 cells per well of a 384 well plate in the presence of varying concentrations of compound (BI-7273, etc.) before measuring viability via cellular ATP levels using the cell titer glow assay[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Martin LJ, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26;59(10):4462-75.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Nevirapine(Synonyms: 奈韦拉平; BI-RG 587; NSC 641530; NVP)

发表于由

Nevirapine (Synonyms: 奈韦拉平; BI-RG 587; NSC 641530; NVP) 纯度: 99.01%

Nevirapine (BI-RG 587) 是用于研究 HIV/AIDS 的 HIV-1 逆转录酶非核苷抑制剂，Ki 值为 270 μM。

Nevirapine(Synonyms: 奈韦拉平; BI-RG 587; NSC 641530; NVP)

Nevirapine Chemical Structure

CAS No. : 129618-40-2

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥572 In-stock
10 mg ￥520 In-stock
50 mg ￥1100 In-stock
100 mg ￥1600 In-stock
200 mg ￥2600 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Nevirapine 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Antiviral Compound Library
  • CNS-Penetrant Compound Library
  • Drug Repurposing Compound Library
  • Anti-COVID-19 Compound Library
  • NMPA-Approved Drug Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Rare Diseases Drug Library
  • Children’s Drug Library

生物活性

Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM[1].

IC50 & Target

Ki: 270 μM (HIV-1 reverse transcriptase)[1]
体外研究
(In Vitro)

Nevirapine itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki=270 μM)[1]. Nevirapine has been used as a re-differentiation agent to treat cancers in several human cancer models. At all doses (100, 200, 350, 500 μM) tested, nevirapine significantly inhibits cell proliferation after 48 h treatment. At high dose (500 μM), nevirapine significantly increases the percentage of apoptotic cells compared with control[2]. Nevirapine is a potent and selective inhibitor (IC50=10-100 nM) of the replication of a wide variety of HIV-1 strains in several cellular assays[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Nevirapine is available for use in combination with nucleoside HIV-1 reverse transcriptase inhibitors (e.g., zidovudine, didanosine, etc.). Nevirapine has received FDA approval for use in combination with HIV-1 protease inhibitors (e.g., saquinavir, ritonavir, indinavir, etc.). In humans, nevirapine is eliminated primarily in the urine as glucuronide conjugates of 2-, 3-, 8-, and 12-hydroxynevirapine[1]. Nevirapine is completely absorbed in both sexes of mouse, rat, rabbit, monkey, and chimpanzee. Nevirapine is extensively metabolized in both sexes of all animal species studied[4]. Nevirapine (9 mg/kg, 18 mg/kg and 36 mg/kg) shows significant reduction in ulcer severity score and ulcer index as compared to the control[5]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

266.30

Formula

C15H14N4O
CAS 号

129618-40-2
中文名称

奈韦拉平；萘维拉平；那韦拉平；奈韦那平；萘韦拉平
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 14.29 mg/mL (53.66 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7552 mL 18.7758 mL 37.5516 mL
5 mM 0.7510 mL 3.7552 mL 7.5103 mL
10 mM 0.3755 mL 1.8776 mL 3.7552 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.43 mg/mL (5.37 mM); Clear solution

    此方案可获得 ≥ 1.43 mg/mL (5.37 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1.43 mg/mL (5.37 mM); Clear solution

    此方案可获得 ≥ 1.43 mg/mL (5.37 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Erickson DA, et al. Characterization of the in vitro biotransformation of the HIV-1 reverse transcriptase inhibitornevirapine by human hepatic cytochromes P-450. Drug Metab Dispos. 1999 Dec;27(12):1488-95.

    [2]. Dong JJ, et al. In vitro evaluation of the therapeutic potential of nevirapine in treatment of human thyroid anaplastic carcinoma. Mol Cell Endocrinol. 2013 May 6;370(1-2):113-8.

    [3]. Merluzzi VJ, et al. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science. 1990 Dec 7;250(4986):1411-3.

    [4]. Riska PS, et al. Biotransformation of nevirapine, a non-nucleoside HIV-1 reverse transcriptase inhibitor, in mice, rats, rabbits, dogs, monkeys, and chimpanzees. Drug Metab Dispos. 1999 Dec;27(12):1434-47.

    [5]. Onasanwo SA, et al. Evaluation of anti-ulcerogenic and ulcer-healing activities of nevirapine in rats. Afr J Med Med Sci. 2015 Sep;44(3):251-9.
Cell Assay
[2]

FRO cells are seeded into 96-well culture plates at 10,000 cells/well. Cells are treated with different doses of nevirapine (0, 100, 200, 350 and 500 μM) for 48 h. MTT dye (5 mg/mL) is added to each well for additional 4 h, and the reaction is then stopped by the addition of DMSO. Optical density is measured at 490 nm on a multi-well plate reader[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[4]

Rats: Nevirapine and [14C] Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1, v/v) with mild heating. The concentration of drug in suspension is 2 mg/mL (20 mg/kg, 26 μCi) for oral dosing to rats and 6.7 mg/mL (20.3 mg/kg, 10 μCi males, 8.9 μCi females) for intraduodenal administration to rats before bile collection. The i.v. dose is administered to rats (1.1 mg/kg, 20 μCi) as a solution in 20% ethanol/80% saline[4].

Mice: Nevirapine and [14C] Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1, v/v) with mild heating. The concentration of drug in suspension is 2 mg/mL (20 mg/kg, 2.5 μCi) with a specific activity of 5.55 μCi/mg for oral dosing to mice[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Erickson DA, et al. Characterization of the in vitro biotransformation of the HIV-1 reverse transcriptase inhibitornevirapine by human hepatic cytochromes P-450. Drug Metab Dispos. 1999 Dec;27(12):1488-95.

    [2]. Dong JJ, et al. In vitro evaluation of the therapeutic potential of nevirapine in treatment of human thyroid anaplastic carcinoma. Mol Cell Endocrinol. 2013 May 6;370(1-2):113-8.

    [3]. Merluzzi VJ, et al. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science. 1990 Dec 7;250(4986):1411-3.

    [4]. Riska PS, et al. Biotransformation of nevirapine, a non-nucleoside HIV-1 reverse transcriptase inhibitor, in mice, rats, rabbits, dogs, monkeys, and chimpanzees. Drug Metab Dispos. 1999 Dec;27(12):1434-47.

    [5]. Onasanwo SA, et al. Evaluation of anti-ulcerogenic and ulcer-healing activities of nevirapine in rats. Afr J Med Med Sci. 2015 Sep;44(3):251-9.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Nevirapine(Synonyms: 奈韦拉平; BI-RG 587; NSC 641530; NVP)

发表于由

Nevirapine (Synonyms: 奈韦拉平; BI-RG 587; NSC 641530; NVP) 纯度: 99.01%

Nevirapine (BI-RG 587) 是用于研究 HIV/AIDS 的 HIV-1 逆转录酶非核苷抑制剂，Ki 值为 270 μM。

Nevirapine(Synonyms: 奈韦拉平; BI-RG 587; NSC 641530; NVP)

Nevirapine Chemical Structure

CAS No. : 129618-40-2

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥572 In-stock
10 mg ￥520 In-stock
50 mg ￥1100 In-stock
100 mg ￥1600 In-stock
200 mg ￥2600 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Nevirapine 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Antiviral Compound Library
  • CNS-Penetrant Compound Library
  • Drug Repurposing Compound Library
  • Anti-COVID-19 Compound Library
  • NMPA-Approved Drug Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Rare Diseases Drug Library
  • Children’s Drug Library

生物活性

Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM[1].

IC50 & Target

Ki: 270 μM (HIV-1 reverse transcriptase)[1]
体外研究
(In Vitro)

Nevirapine itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki=270 μM)[1]. Nevirapine has been used as a re-differentiation agent to treat cancers in several human cancer models. At all doses (100, 200, 350, 500 μM) tested, nevirapine significantly inhibits cell proliferation after 48 h treatment. At high dose (500 μM), nevirapine significantly increases the percentage of apoptotic cells compared with control[2]. Nevirapine is a potent and selective inhibitor (IC50=10-100 nM) of the replication of a wide variety of HIV-1 strains in several cellular assays[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Nevirapine is available for use in combination with nucleoside HIV-1 reverse transcriptase inhibitors (e.g., zidovudine, didanosine, etc.). Nevirapine has received FDA approval for use in combination with HIV-1 protease inhibitors (e.g., saquinavir, ritonavir, indinavir, etc.). In humans, nevirapine is eliminated primarily in the urine as glucuronide conjugates of 2-, 3-, 8-, and 12-hydroxynevirapine[1]. Nevirapine is completely absorbed in both sexes of mouse, rat, rabbit, monkey, and chimpanzee. Nevirapine is extensively metabolized in both sexes of all animal species studied[4]. Nevirapine (9 mg/kg, 18 mg/kg and 36 mg/kg) shows significant reduction in ulcer severity score and ulcer index as compared to the control[5]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

266.30

Formula

C15H14N4O
CAS 号

129618-40-2
中文名称

奈韦拉平；萘维拉平；那韦拉平；奈韦那平；萘韦拉平
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 14.29 mg/mL (53.66 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7552 mL 18.7758 mL 37.5516 mL
5 mM 0.7510 mL 3.7552 mL 7.5103 mL
10 mM 0.3755 mL 1.8776 mL 3.7552 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.43 mg/mL (5.37 mM); Clear solution

    此方案可获得 ≥ 1.43 mg/mL (5.37 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1.43 mg/mL (5.37 mM); Clear solution

    此方案可获得 ≥ 1.43 mg/mL (5.37 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Erickson DA, et al. Characterization of the in vitro biotransformation of the HIV-1 reverse transcriptase inhibitornevirapine by human hepatic cytochromes P-450. Drug Metab Dispos. 1999 Dec;27(12):1488-95.

    [2]. Dong JJ, et al. In vitro evaluation of the therapeutic potential of nevirapine in treatment of human thyroid anaplastic carcinoma. Mol Cell Endocrinol. 2013 May 6;370(1-2):113-8.

    [3]. Merluzzi VJ, et al. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science. 1990 Dec 7;250(4986):1411-3.

    [4]. Riska PS, et al. Biotransformation of nevirapine, a non-nucleoside HIV-1 reverse transcriptase inhibitor, in mice, rats, rabbits, dogs, monkeys, and chimpanzees. Drug Metab Dispos. 1999 Dec;27(12):1434-47.

    [5]. Onasanwo SA, et al. Evaluation of anti-ulcerogenic and ulcer-healing activities of nevirapine in rats. Afr J Med Med Sci. 2015 Sep;44(3):251-9.
Cell Assay
[2]

FRO cells are seeded into 96-well culture plates at 10,000 cells/well. Cells are treated with different doses of nevirapine (0, 100, 200, 350 and 500 μM) for 48 h. MTT dye (5 mg/mL) is added to each well for additional 4 h, and the reaction is then stopped by the addition of DMSO. Optical density is measured at 490 nm on a multi-well plate reader[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[4]

Rats: Nevirapine and [14C] Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1, v/v) with mild heating. The concentration of drug in suspension is 2 mg/mL (20 mg/kg, 26 μCi) for oral dosing to rats and 6.7 mg/mL (20.3 mg/kg, 10 μCi males, 8.9 μCi females) for intraduodenal administration to rats before bile collection. The i.v. dose is administered to rats (1.1 mg/kg, 20 μCi) as a solution in 20% ethanol/80% saline[4].

Mice: Nevirapine and [14C] Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1, v/v) with mild heating. The concentration of drug in suspension is 2 mg/mL (20 mg/kg, 2.5 μCi) with a specific activity of 5.55 μCi/mg for oral dosing to mice[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Erickson DA, et al. Characterization of the in vitro biotransformation of the HIV-1 reverse transcriptase inhibitornevirapine by human hepatic cytochromes P-450. Drug Metab Dispos. 1999 Dec;27(12):1488-95.

    [2]. Dong JJ, et al. In vitro evaluation of the therapeutic potential of nevirapine in treatment of human thyroid anaplastic carcinoma. Mol Cell Endocrinol. 2013 May 6;370(1-2):113-8.

    [3]. Merluzzi VJ, et al. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science. 1990 Dec 7;250(4986):1411-3.

    [4]. Riska PS, et al. Biotransformation of nevirapine, a non-nucleoside HIV-1 reverse transcriptase inhibitor, in mice, rats, rabbits, dogs, monkeys, and chimpanzees. Drug Metab Dispos. 1999 Dec;27(12):1434-47.

    [5]. Onasanwo SA, et al. Evaluation of anti-ulcerogenic and ulcer-healing activities of nevirapine in rats. Afr J Med Med Sci. 2015 Sep;44(3):251-9.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

BI-6015

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BI-6015  纯度: 98.67%

BI-6015 是一种肝细胞核因子 4α (HNF4α) 拮抗剂，可抑制已知 HNF4α 靶基因的表达。BI6015 通过 HNF4α 拮抗作用抑制胰岛素启动子活性。BI-6015 可用于癌症和糖尿病的研究。

BI-6015

BI-6015 Chemical Structure

CAS No. : 93987-29-2

规格 价格 是否有货 数量
5 mg ￥700 In-stock
10 mg ￥1200 In-stock
25 mg ￥3700 In-stock
50 mg ￥5400 In-stock
100 mg ￥8700 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

BI-6015 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Diabetes Related Compound Library

生物活性

BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes[1].

IC50 & Target

hepatocyte nuclear factor 4α (HNF4α)[1]
体外研究
(In Vitro)

BI-6015 (1.25-20 μM; 24-72 h) is cytotoxic to human hepatocellular carcinoma (HCC)[1].
BI-6015 (2.5-10 μM; 5-48 h) inhibits HNF4α gene expression in HepG2 cells[1].
BI-6015 (5 μM; 3 d) induces hepatic steatosis in primary murine hepatocytes[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Hep3B-Luc cells and primary hepatocytes
Concentration: 1.25, 2.5, 5, 10, 20 μM
Incubation Time: 24, 48, 72 hours
Result: Was markedly toxic to Hep3B cells but spared primary hepatocytes.

体内研究
(In Vivo)

BI-6015 (10-30 mg/kg; i.p. once daily for 5 days) induces loss of HNF4α expression and hepatic steatosis in mice[1].
BI-6015 (10-30 mg/kg; i.p. daily or every other day for 20-57 days) induces apoptosis in a human hepatocellular carcinoma mouse model[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

331.35

Formula

C15H13N3O4S
CAS 号

93987-29-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (150.90 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0180 mL 15.0898 mL 30.1796 mL
5 mM 0.6036 mL 3.0180 mL 6.0359 mL
10 mM 0.3018 mL 1.5090 mL 3.0180 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.54 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Kiselyuk A, et, al. HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter. Chem Biol. 2012 Jul 27;19(7):806-18.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

BI-4464

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BI-4464  纯度: 99.27%

BI-4464 是具有高度选择性的，ATP竞争性的、PTK2/FAK 的抑制剂，其IC50 值为 17 nM。是可用于PROTAC 降解剂的一个PTK2 配体。

BI-4464

BI-4464 Chemical Structure

CAS No. : 1227948-02-8

规格 价格 是否有货 数量
5 mg ￥3700 In-stock
10 mg ￥5950 In-stock
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

BI-4464 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. A PTK2 ligand for PROTAC[1].

IC50 & Target

IC50: 17 nM (PTK2/FAK)[1].
分子量

555.55

Formula

C28H28F3N5O4
CAS 号

1227948-02-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 16.67 mg/mL (30.01 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8000 mL 9.0001 mL 18.0002 mL
5 mM 0.3600 mL 1.8000 mL 3.6000 mL
10 mM 0.1800 mL 0.9000 mL 1.8000 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Popow J, et al. Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions. J Med Chem. 2019 Mar 14;62(5):2508-2520.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Bio-Tek宝特 ELx808IU酶标仪

发表于由
Bio-Tek宝特 ELx808IU酶标仪

Bio-Tek宝特 ELx808IU酶标仪

  • 商品品牌： Bio-Tek宝特
    商品编号：ELX808IU
  • 商品价格： 请与我们联系

    • Bio-Tek宝特 ELx808IU酶标仪-Bio-Tek宝特-ELX808IU

    • 类型:滤光片式酶标仪
    • 波长范围:340-850nm
    • 滤光片位:6个
    • 内置打印机:无
    • 孵育器:有
    • 品牌属性:进口
    生命科学仪器|||生化免疫|||酶标仪|||Bio-Tek宝特ELx808IU酶标仪
    自动酶标分析仪 酶联免疫检测仪 340-850nm 4个 无 有 进口

    Bio-Tek宝特 ELx808IU酶仪

    ELx808IU™ 酶标仪延续了 BioTek 提供最高规格酶标仪的一贯传统，具有精度高、准确性好、重复性强的特点，在数据处理和分析方面具有出色的灵活性。

    主要特点：
    广泛的机载数据分析

    数据转换公式
    分析和控制验证
    曲线拟合选项：直线、四点对数曲线、二点对数曲线、三次方曲线、二次方曲线、三次样条函数曲线、逐点连线

    　快速动力学测试

    测试间隔时间短至 6 秒
    可针对凝集实验进行线性孔扫描

    动力学速率、R2 或起始时间报告（无需 PC）

    　4-Zone™ 温度控制

    孵育温度达 50℃

    改良的酶动力学实验重复性

    通过独立监控的加热器来增强一致性

    独特的加热追踪/传送设计最小化蒸发和边缘效应

    　绝佳的光学设计

    采用交错的光学设计，有消除光通道间的色度亮度干扰

    参考通道循环光信号，可统一通道间的信号

    商品属性

    • 类型:滤光片式酶标仪
    • 波长范围:340-850nm
    • 滤光片位:6个
    • 内置打印机:无
    • 孵育器:有
    • 品牌属性:进口
    商品属性
    商品名称 Bio-Tek宝特 ELx808IU酶标仪-ELX808IU-Bio-Tek宝特
    型号 ELX808IU
    类别 生命科学仪器|||生化免疫|||酶标仪|||Bio-Tek宝特ELx808IU酶标仪
    品牌 Bio-Tek宝特
    品牌简介 Bio-Tek宝特
    关键字 自动酶标分析仪 酶联免疫检测仪 340-850nm 4个 无 有 进口,曲线,动力学,对数,波长,通道,光学

    Bio-Tek宝特 ELx808IU酶标仪

    Spectronics TVD-1000R双光源(BIO-Vision)系列紫外透射仪

    发表于由
    Spectronics TVD-1000R双光源(BIO-Vision)系列紫外透射仪

    Spectronics TVD-1000R双光源(BIO-Vision)系列紫外透射仪

  • 商品品牌： Spectronics
    商品编号：TVD-1000R
  • 商品价格： 请与我们联系

    • Spectronics TVD-1000R双光源(BIO-Vision)系列紫外透射仪-Spectronics-TVD-1000R

    • 类型:台式
    • 光源:透射
    • 波长:单波长单波长
    • 品牌属性:进口
    生命科学仪器|||电泳成像|||紫外分析仪|||SpectronicsTVD-1000R双光源(BIO-Vision)系列紫外透射仪
    紫外透射检测仪/台 紫外分析仪

    TVD-1000R双光源(BIO-Vision)系列紫外透射仪功能特点：

    ※ 可选择固定或可调强度型号–共29种型号供选择

    ※ 各种UV 紫外线波长组合(312nm, 254nm 及/或365nm)及白光

    ※ 可调高强度UV紫外透射仪提供最高强度及最长的样品准备时间

    ※ 高强度紫外线强度产生明亮的荧光反应及高清晰度。

    ※ 特殊的散射屏确保优异的照射均匀性，消除光条纹。

    ※ 可与照相/视频装置配合使用

    –

    LONGLIFE 滤色片寿命测试；

    在中波紫外线强度达11,000 µW/cm2 下测得

    没有光条纹(左图)及有光条纹(右图)

    		 详细描述：

    出众的性能

    超高的紫外强度及均匀照射，即使是微量的DNA也能发现。

    LONGLIFE™ 长寿命滤色片

    抑制日晒，寿命是普通滤色片的50倍，节省成本。

    强劲的冷却风扇

    使滤色片维持在低温状态，防止紫外强度下降及由于表面热量聚集而损坏样品。

    特殊散射屏

    所有312nm及365nm型号的滤色片下面都配有可拆除散射屏，确保出众的光照射，

    消除灯管轮廓产生的光条纹 (见左图)。

    最长的样品准备时间及最高的灵敏度！

    在准备阶段，为获得最大的样品保护，Spectroline TV-系列可调强度UV紫外透射仪强度从100%–20%连续可调 (TVD-1000R 双光源透射仪为100%-50%)。

    光滑，易于清洁的滤色片架

    减少凝胶损坏及污染。

    自动计时关机

    防止过量紫外曝光(TC-及TL-系列)。

    将图片损坏降到最低

    Spectroline 312nm 透射仪没有254nm紫外辐射，从而将图片损坏降到最低程度。

    由于样品时间更长，因而您的测试变得更快、更轻松。

    UV紫外防护盖

    防止有害的紫外线对人的照射。UV-紫外防护盖可防止操作人员紫外暴露。

    防止意外掉到滤色片的物体对滤色片造成损害。

    商品属性

    • 类型:台式
    • 光源:透射
    • 波长:单波长单波长
    • 品牌属性:进口
    商品属性
    商品名称 Spectronics TVD-1000R双光源(BIO-Vision)系列紫外透射仪-TVD-1000R-Spectronics
    型号 TVD-1000R
    类别 生命科学仪器|||电泳成像|||紫外分析仪|||SpectronicsTVD-1000R双光源(BIO-Vision)系列紫外透射仪
    品牌 Spectronics
    品牌简介 Spectronics
    关键字 紫外透射检测仪/台 紫外分析仪,可调,强度,样品,条纹,紫外线,波长

    Spectronics TVD-1000R双光源(BIO-Vision)系列紫外透射仪

    Biohit百得 Genex手动可调式移液器0.5-10ul（720000DL）

    发表于由
    Biohit百得 Genex手动可调式移液器0.5-10ul（720000DL）

    Biohit百得 Genex手动可调式移液器0.5-10ul（720000DL）

  • 商品品牌： Biohit芬兰百得
    商品编号：720000DL
  • 商品价格： 请与我们联系

    • Biohit百得 Genex手动可调式移液器0.5-10ul（720000DL）-Biohit芬兰百得-720000DL

    • 移液方式:手动可调
    • 灭菌方式:整支灭菌
    • 量程:100ul以下
    • 品牌属性:进口
    实验室耗材|||移液处理|||单道移液器|||Biohit百得Genex手动可调式移液器0.5-10ul（720000DL）
    移液器 移液枪 进口

     

    Biohit百得 Genex手动可调式移液器（720000DL）

     

    Genex系列可变容量单道手动移液器

    精确和准确的样品及试剂的转移，对实现可靠的分析结果

    是至关重要的。液体处理产品移液器已广泛用于在全球

    许多重要 和常规的领域。为此，芬兰百得公司，推出一

    系列符合中国国情的新款系列Genex手动可变容量移液

    器。除保留了芬兰百得 的国际标准制造等一系列特点

    外，更具有最佳的性能价格比。

    Genex 系列可变容量单道手动移液器的特点

    Genex 系列手动移液器具有平滑的活塞运动和较轻的重量使操作
    易于校准和保养，零件少，拆卸方便灵活；
    高弹性的吸头连接锥体确保密封，具有良好的化学耐受性；
    最佳的性能价格比。

    的舒适性及准确性得以实现，可调容量覆盖了0.05μl～5,000μl的

    范围，其适合于众多的应用领域。

    轻便的人体工程学设计；

    极轻巧的移液和吸头弹出操作性能；

    具有锁扣设计的量程锁定；

    清晰的数字显示，一目了然；

    良好宽范围的吸头适配性；

    百得（Biohit）产品已通过下列资质认证：

    商品属性

    • 移液方式:手动可调
    • 灭菌方式:整支灭菌
    • 量程:100ul以下
    • 品牌属性:进口
    商品属性
    商品名称 Biohit百得 Genex手动可调式移液器0.5-10ul（720000DL）-720000DL-Biohit芬兰百得
    型号 720000DL
    类别 实验室耗材|||移液处理|||单道移液器|||Biohit百得Genex手动可调式移液器0.5-10ul（720000DL）
    品牌 Biohit芬兰百得
    品牌简介 Biohit芬兰百得
    关键字 移液器 移液枪 进口,吸头,系列,芬兰,容量,调式,性能

    Biohit百得 Genex手动可调式移液器0.5-10ul（720000DL）

    BI-9321

    发表于由

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

    BI-9321 

    BI-9321 是一种有效的，选择性的，具有细胞活性的 NSD3-PWWP1 拮抗剂，Kd 值为 166 nM。BI-9321 对 NSD2-PWWP1 和 NSD3-PWWP2 无效。BI-9321 在 U2OS 细胞中特异性破坏 NSD3-PWWP1 与组蛋白相互作用，IC50 为 1.2 μM。

    BI-9321

    BI-9321 Chemical Structure

    CAS No. : 2387510-86-1

    规格 是否有货
    100 mg   询价  
    250 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    BI-9321 的其他形式现货产品:

    BI-9321 trihydrochloride

    生物活性

    BI-9321 is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells[1].

    IC50 & Target

    Kd: 166 nM (NSD3-PWWP1)[1]
    体外研究
    (In Vitro)

    BI-9321 is targeting the methyl-lysine binding site of the PWWP1 domain with sub-micromolar in vitro activity and cellular target engagement at 1 µM. As a single agent, BI-9321 downregulates Myc messenger RNA expression and reduces proliferation in MOLM-13 cells[1].

    Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    360.43

    Formula

    C22H21FN4
    CAS 号

    2387510-86-1
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    参考文献

    • [1]. Böttcher J, et al. Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3. Nat Chem Biol. 2019 Aug;15(8):822-829.

    所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

    BI-9321

    发表于由

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

    BI-9321 

    BI-9321 是一种有效的，选择性的，具有细胞活性的 NSD3-PWWP1 拮抗剂，Kd 值为 166 nM。BI-9321 对 NSD2-PWWP1 和 NSD3-PWWP2 无效。BI-9321 在 U2OS 细胞中特异性破坏 NSD3-PWWP1 与组蛋白相互作用，IC50 为 1.2 μM。

    BI-9321

    BI-9321 Chemical Structure

    CAS No. : 2387510-86-1

    规格 是否有货
    100 mg   询价  
    250 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    BI-9321 的其他形式现货产品:

    BI-9321 trihydrochloride

    生物活性

    BI-9321 is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells[1].

    IC50 & Target

    Kd: 166 nM (NSD3-PWWP1)[1]
    体外研究
    (In Vitro)

    BI-9321 is targeting the methyl-lysine binding site of the PWWP1 domain with sub-micromolar in vitro activity and cellular target engagement at 1 µM. As a single agent, BI-9321 downregulates Myc messenger RNA expression and reduces proliferation in MOLM-13 cells[1].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    360.43

    Formula

    C22H21FN4
    CAS 号

    2387510-86-1
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    参考文献

    • [1]. Böttcher J, et al. Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3. Nat Chem Biol. 2019 Aug;15(8):822-829.

    所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

    BI-9321

    发表于由

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

    BI-9321 

    BI-9321 是一种有效的，选择性的，具有细胞活性的 NSD3-PWWP1 拮抗剂，Kd 值为 166 nM。BI-9321 对 NSD2-PWWP1 和 NSD3-PWWP2 无效。BI-9321 在 U2OS 细胞中特异性破坏 NSD3-PWWP1 与组蛋白相互作用，IC50 为 1.2 μM。

    BI-9321

    BI-9321 Chemical Structure

    CAS No. : 2387510-86-1

    规格 是否有货
    100 mg   询价  
    250 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    BI-9321 的其他形式现货产品:

    BI-9321 trihydrochloride

    生物活性

    BI-9321 is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells[1].

    IC50 & Target

    Kd: 166 nM (NSD3-PWWP1)[1]
    体外研究
    (In Vitro)

    BI-9321 is targeting the methyl-lysine binding site of the PWWP1 domain with sub-micromolar in vitro activity and cellular target engagement at 1 µM. As a single agent, BI-9321 downregulates Myc messenger RNA expression and reduces proliferation in MOLM-13 cells[1].

    Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    360.43

    Formula

    C22H21FN4
    CAS 号

    2387510-86-1
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    参考文献

    • [1]. Böttcher J, et al. Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3. Nat Chem Biol. 2019 Aug;15(8):822-829.

    所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

    JET BIOFIL洁特 一次性塑料离心管 50ml （CFT100500）

    发表于由
    JET BIOFIL洁特 一次性塑料离心管 50ml （CFT100500）
    JET BIOFIL洁特 一次性塑料离心管 50ml （CFT100500）
    JET BIOFIL洁特 一次性塑料离心管 50ml （CFT100500）

    JET BIOFIL洁特 一次性塑料离心管 50ml （CFT100500）

  • 商品品牌： JET洁特
    商品编号：CFT100500
  • 商品价格： 请与我们联系

    • JET BIOFIL洁特 一次性塑料离心管 50ml （CFT100500）-JET洁特-CFT100500

    • 产品类型:微量
    • 灭菌性质:未灭菌
    • 容量:50ml
    • 品牌属性:国产
    实验室耗材|||过滤离心|||离心管|||JETBIOFIL洁特一次性塑料离心管50ml（CFT100500）
    塑料离心管 50ml

    JET BIOFIL洁特 一次性微量离心管 50ml （CFT100500）

    产品特性：

    JET BIOFIL®一次性塑料离心管由高质量的透明高分子材料聚丙烯（PP）制成，已广泛应用于多种实验的操作中，满足生物分析级要求。

    ◎ 2种容量规格可选：15和50mL，2种管底类型可选：圆锥形和可立式底

    ◎ 管体内外表面光滑，色泽均匀

    ◎ 外表面印有清晰黑色刻度、可写入文字的白色区域，耐三氯甲烷

    ◎ 最大的RCF：9,400g（圆锥形底管）；RCF：6,000g（可立式底管）

    ◎ 可承受温度范围：-80℃—121℃

    ◎ 经过严格地泄漏测试

    ◎ 伽玛射线消毒灭菌或未消毒可选

    小贴士：

    离心技术在生物科学，特别是生物化学和分子生物学研究领域，已得到十分广泛的应用，每个生物化学和分子生物学实验室都要准备多种型式的离心机。离

    心技术主要用于各种生物样品的分离和制备，生物样品悬浮液盛放在离心管中在高速旋转下，由于巨大的离心力作用，使悬浮的微小颗粒（如细胞器、生物大分

    子的沉淀等）以一定的速度沉降，从而与溶液得以分离。

    基本原理：

    当一个粒子（生物大分子或细胞器）在高速旋转下受到离心力作用时此离心力“F”由下式定义，

    即： F = ma = mω2 r

    a — 粒子旋转的加速度， m — 沉降粒子的有效质量，ω—粒子旋转的角速度， r—粒子的旋转半径( cm )。

    通常离心力常用地球引力的倍数来表示，因而称为相对离心力 “ RCF ”。

    或者用数字乘“g”来表示例如25000×g，则表示相对离心力为25000。

    商品属性

    • 产品类型:微量
    • 灭菌性质:未灭菌
    • 容量:50ml
    • 品牌属性:国产
    商品属性
    商品名称 JET BIOFIL洁特 一次性塑料离心管 50ml （CFT100500）-CFT100500-JET洁特
    型号 CFT100500
    类别 实验室耗材|||过滤离心|||离心管|||JETBIOFIL洁特一次性塑料离心管50ml（CFT100500）
    品牌 JET洁特
    品牌简介 JET洁特
    关键字 塑料离心管 50ml,离心管,离心力,粒子,塑料,生物,细胞器

    JET BIOFIL洁特 一次性塑料离心管 50ml （CFT100500） JET BIOFIL洁特 一次性塑料离心管 50ml （CFT100500） JET BIOFIL洁特 一次性塑料离心管 50ml （CFT100500）

    BI-9321 trihydrochloride

    发表于由

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

    BI-9321 trihydrochloride  纯度: 98.89%

    BI-9321 trihydrochloride 是一种有效的，选择性的，具有细胞活性的 NSD3-PWWP1 拮抗剂，Kd 值为 166 nM。BI-9321 对 NSD2-PWWP1 和 NSD3-PWWP2 无效。BI-9321 trihydrochloride 在 U2OS 细胞中特异性破坏 NSD3-PWWP1 与组蛋白相互作用，IC50 为 1.2 μM。

    BI-9321 trihydrochloride

    BI-9321 trihydrochloride Chemical Structure

    CAS No. : 2387510-87-2

    规格 价格 是否有货 数量
    Free Sample (0.1-0.5 mg)   Apply now  
    10 mM * 1 mL in DMSO ￥1430 In-stock
    5 mg ￥1300 In-stock
    10 mg ￥2300 In-stock
    25 mg ￥4500 In-stock
    50 mg ￥7600 In-stock
    100 mg ￥12000 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    BI-9321 trihydrochloride 相关产品

    •相关化合物库:

    • Bioactive Compound Library Plus
    • Epigenetics Compound Library
    • Histone Modification Research Compound Library
    • Anti-Cancer Compound Library
    • Anti-Blood Cancer Compound Library
    • Targeted Diversity Library

    生物活性

    BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells[1].

    IC50 & Target

    Kd: 166 nM (NSD3-PWWP1)[1]
    体外研究
    (In Vitro)

    BI-9321 trihydrochloride is targeting the methyl-lysine binding site of the PWWP1 domain with sub-micromolar in vitro activity and cellular target engagement at 1 µM. As a single agent, BI-9321 trihydrochloride downregulates Myc messenger RNA expression and reduces proliferation in MOLM-13 cells[1].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    469.81

    Formula

    C22H24Cl3FN4
    CAS 号

    2387510-87-2
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, stored under nitrogen, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
    溶解性数据
    In Vitro: 

    DMSO : 250 mg/mL (532.13 mM; Need ultrasonic)

    H2O : 25 mg/mL (53.21 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1285 mL 10.6426 mL 21.2852 mL
    5 mM 0.4257 mL 2.1285 mL 4.2570 mL
    10 mM 0.2129 mL 1.0643 mL 2.1285 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 25 mg/mL (53.21 mM); Clear solution

      此方案可获得 ≥ 25 mg/mL (53.21 mM，饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 250.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 25 mg/mL (53.21 mM); Clear solution

      此方案可获得 ≥ 25 mg/mL (53.21 mM，饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 250.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
    • 3.

      请依序添加每种溶剂： 10% DMSO    90% corn oil

      Solubility: ≥ 25 mg/mL (53.21 mM); Clear solution

      此方案可获得 ≥ 25 mg/mL (53.21 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例，取 100 μL 250.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献

    • [1]. Böttcher J, et al. Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3. Nat Chem Biol. 2019 Aug;15(8):822-829.

    所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

    BI-2852

    发表于由

    BI-2852  纯度: 98.74%

    BI-2852 是基于药物结构设计的 switch SI/II 口袋的 KRAS 抑制剂，其通过基于结构的药物设计具有纳摩尔亲和力。 BI-2852 在机理上不同于共价 KRASG12C 抑制剂 (结合 switch II)，与活性 KRASG12D 结合强度是与 KRAS wt 的 10 倍 (740 nM vs 7.5 μM)。BI-2852 阻断 GEF，GAP 和效应子与 KRAS 的相互作用，导致下游信号传导的抑制和 KRAS 突变细胞中的抗增殖作用。

    BI-2852

    BI-2852 Chemical Structure

    CAS No. : 2375482-51-0

    规格 价格 是否有货 数量
    10 mM * 1 mL in DMSO ￥3980 In-stock
    5 mg ￥3500 In-stock
    10 mg ￥5500 In-stock
    50 mg ￥16500 In-stock
    100 mg ￥29000 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    BI-2852 相关产品

    •相关化合物库:

    • Covalent Screening Library Plus
    • Bioactive Compound Library Plus
    • GPCR/G Protein Compound Library
    • Kinase Inhibitor Library
    • Anti-Cancer Compound Library
    • Covalent Screening Library
    • Ferroptosis Compound Library
    • Glutamine Metabolism Compound Library
    • Anti-Lung Cancer Compound Library
    • Anti-Pancreatic Cancer Compound Library
    • Anti-Blood Cancer Compound Library
    • Angiogenesis Related Compound Library
    • Anti-Liver Cancer Compound Library
    • Anti-Colorectal Cancer Compound Library

    生物活性

    BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells[1].

    IC50 & Target[1]

    KRAS(G12C)

    450 nM (IC50)

    KRAS(G12C)

    750 nM (Kd)

    体外研究
    (In Vitro)

    BI-2852 (Compound 1) (10 nM-10 µM; 2 hours) shows a dose-dependent pERK modulation and antiproliferative effect at EC50s of 5.8 µM and 6.7 µM in soft agar and low serum conditions in NCI-H358 cells[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    516.59

    Formula

    C31H28N6O2
    CAS 号

    2375482-51-0
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
    溶解性数据
    In Vitro: 

    DMSO : 55 mg/mL (106.47 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9358 mL 9.6789 mL 19.3577 mL
    5 mM 0.3872 mL 1.9358 mL 3.8715 mL
    10 mM 0.1936 mL 0.9679 mL 1.9358 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (4.84 mM，饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (4.84 mM，饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
    • 3.

      请依序添加每种溶剂： 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (4.84 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献

    • [1]. Kessler D, et al. Drugging an undruggable pocket on KRAS. Proc Natl Acad Sci U S A. 2019 Aug 6; 116(32):15823-15829.

      [2]. Dirk Kessler, et al. Drugging all RAS isoforms with one pocket. FUTURE MEDICINAL CHEMISTRY

    BI-3406

    发表于由

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

    BI-3406  纯度: 99.79%

    BI-3406 (compound I-6) 是一种具有口服活性，高效且选择性的 KRAS-SOS1 抑制剂，可抑制 KRAS 与 SOS1 之间相互作用，IC50 为 6 nM。BI-3406 有效地减少了 GTP 加载的 KRAS 的形成，并抑制了 MAPK 信号通路。BI-3406 具有抗癌活性。

    BI-3406

    BI-3406 Chemical Structure

    CAS No. : 2230836-55-0

    规格 价格 是否有货 数量
    10 mM * 1 mL in DMSO ￥3560 In-stock
    5 mg ￥3500 In-stock
    10 mg ￥6500 In-stock
    100 mg ￥19500 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    BI-3406 相关产品

    •相关化合物库:

    • Covalent Screening Library Plus
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    • GPCR/G Protein Compound Library
    • Immunology/Inflammation Compound Library
    • Kinase Inhibitor Library
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    • Anti-Cancer Compound Library
    • Covalent Screening Library
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    • Anti-Lung Cancer Compound Library
    • Anti-Pancreatic Cancer Compound Library
    • Anti-Blood Cancer Compound Library
    • Neurodegenerative Disease-related Compound Library
    • Angiogenesis Related Compound Library
    • Anti-Liver Cancer Compound Library
    • Anti-Colorectal Cancer Compound Library

    生物活性

    BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity[1][2].

    IC50 & Target[1]

    KRAS-SOS1

    6 nM (IC50)

    体外研究
    (In Vitro)

    BI-3406 is an inhibitor of the interaction between KRAS and its Guanine Nucleotide Exchange Factor (GEF) SOS1. BI-3406 does not block the interaction of KRAS with SOS2 but elicits activity on a broad panel of KRAS oncogenic variants, including all major G12 and G13 oncoproteins. Down-modulation of this signaling cascade by BI-3406 in KRAS G12 or G13 mutant cells effectively limits cell proliferation[2].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    462.46

    Formula

    C23H25F3N4O3
    CAS 号

    2230836-55-0
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
    溶解性数据
    In Vitro: 

    Ethanol : 100 mg/mL (216.23 mM; Need ultrasonic)

    DMSO : 100 mg/mL (216.23 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1623 mL 10.8117 mL 21.6235 mL
    5 mM 0.4325 mL 2.1623 mL 4.3247 mL
    10 mM 0.2162 mL 1.0812 mL 2.1623 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.41 mM，饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (5.41 mM); Clear solution; Need ultrasonic

      此方案可获得 2.5 mg/mL (5.41 mM) 的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
    • 3.

      请依序添加每种溶剂： 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.41 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

    • 4.

      请依序添加每种溶剂： 10% EtOH    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.41 mM，饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

    • 5.

      请依序添加每种溶剂： 10% EtOH    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.41 mM，饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
    • 6.

      请依序添加每种溶剂： 10% EtOH    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.41 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中，混合均匀。

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献

    • [1]. Michael Gmachl, et al. Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors. WO2018115380A1.

      [2]. Marco H Hofmann, et al. Abstract PL06-01: Discovery of BI-3406: A potent and selective SOS1::KRAS inhibitor opens a new approach for treating KRAS-driven tumors. December 2019.

    所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

    BI-882370

    发表于由

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

    BI-882370  纯度: 99.16%

    BI-882370 是一种高效选择性的 RAF 激酶抑制剂，其结合位于 BRAF 激酶的 DFG-out 无活性构象处 (ATP 结合位点)。 BI-882370 抑制 BRAFV600E-mutant, WT BRAF 和 CRAF 激酶的 IC50 值分别为 0.4，0.8 和 0.6 nM。BI-882370 也可以抑制 SRC 家族激酶。

    BI-882370

    BI-882370 Chemical Structure

    CAS No. : 1392429-79-6

    规格 价格 是否有货 数量
    Free Sample (0.1-0.5 mg)   Apply now  
    5 mg ￥950 In-stock
    10 mg ￥1700 In-stock
    50 mg ￥5500 In-stock
    100 mg ￥9700 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    BI-882370 相关产品

    •相关化合物库:

    • Bioactive Compound Library Plus
    • Immunology/Inflammation Compound Library
    • Kinase Inhibitor Library
    • MAPK Compound Library
    • Anti-Cancer Compound Library
    • Oxygen Sensing Compound Library
    • Ferroptosis Compound Library
    • Glutamine Metabolism Compound Library
    • Anti-Lung Cancer Compound Library
    • Anti-Pancreatic Cancer Compound Library
    • Anti-Liver Cancer Compound Library
    • Anti-Colorectal Cancer Compound Library

    生物活性

    BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases[1].

    IC50 & Target[1]

    Braf

    0.6 nM (IC50)

    c-Raf

    0.8 nM (IC50)

    BRafV600E

    0.4 nM (IC50)

    体外研究
    (In Vitro)

    BI-882370 (0.9-6000 nM; 3 days) inhibits the BRAF-mutant human melanoma and colorectal cancer cells proliferation with a EC50 range of 1-10 nM[1].
    BI 882370 (0.1-100 nM, 0.1-3000 nM; 2 hours) results in a reduction of p-MEK1/2, p-ERK1/2 and cyclin D1/D2 expression in BRAFV600E-mutant A375 cells; induces phosphorylation of MEK1/2 and enhanced phosphorylation of ERK1/2 in WT BRO cells (3-300 nM)[1].
    BI 882370 (0.1-100 nM, 0.1-3000 nM; 24 hours) suppresses cyclin D1/D2 expression, induces Kip1/p27 expression at concentrations of 1 nM or higher in BRAFV600E-mutant A375 cells, expression of cyclins D1/D2 or Kip1/p27 is not affected in WT BRO cells[1].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Proliferation Assay[1]

    Cell Line: BRAF-mutant and WT melanoma cell lines (A101D, A375, SK-MEL-28, G-361, and BRO); Colorectal cancer cell lines (COLO 205, HT-29, LS411N, and HCT-116)
    Concentration: 0.9-6000 nM
    Incubation Time: 3 days
    Result: Showed a EC50 range of 1-10 nM in an extended panel of BRAF-mutant human melanoma and colorectal cancer cell; while proliferation of BRAF WT cells was inhibited with EC50 >1 μM.

    Western Blot Analysis[1]

    Cell Line: BRAFV600E-mutant A375 cells; BRAF WT, NRAS-mutant BRO (WT BRO) cells
    Concentration: 0.1-100 nM; 0.1-3000 nM
    Incubation Time: 2 hours; 24 hours
    Result: Resulted in a reduction of phospho-MEK1/2 signals and cyclin D1/D2 expression in BRAFV600E-mutant A375 cells.

    体内研究
    (In Vivo)

    BI-882370 (deliver orally; 25 mg/kg, 50 mg/kg; twice daily; 2 weeks) is efficacious in multiple mouse models of BRAF-mutant melanomas and colorectal carcinomas, shows superior efficacy compared with Vemurafenib, Dabrafenib, or Trametinib[1].
    BI-882370 (deliver orally; 25 mg/kg; twice daily; 40 days) developes resistance within 3 weeks, but resistance is not observed during 5 weeks of second-line therapy in combination with trametinib[1].
    BI-882370 (deliver orally; 60 mg/kg; once daily; 2 weeks) indicates lack of toxicity in terms of clinical chemistry, hematology, pathology, and toxicogenomics in rats[1].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Human melanoma xenografts in nude mice with BRAF-mutant melanomas and colorectal carcinomas cells (A375, COLO 205; G-361, HT-29 cells)[1]
    Dosage: 25 mg/kg; 50 mg/kg
    Administration: Deliver orally; 25 mg/kg, 50 mg/kg; twice daily; 2 weeks
    Result: Regressed tumors partially, upon discontinuation, tumor regrowth was markedly delayed.

    分子量

    569.67

    Formula

    C28H33F2N7O2S
    CAS 号

    1392429-79-6
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 5 mg/mL (8.78 mM; ultrasonic and warming and heat to 60°C)

    H2O : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.7554 mL 8.7770 mL 17.5540 mL
    5 mM 0.3511 mL 1.7554 mL 3.5108 mL
    10 mM — — —

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
    参考文献

    • [1]. Waizenegger IC, et al. A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation. Mol Cancer Ther. 2016 Mar;15(3):354-65.

    所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

    Olmutinib(Synonyms: 奥莫替尼; HM61713, BI 1482694)

    发表于由

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

    Olmutinib (Synonyms: 奥莫替尼; HM61713, BI 1482694) 纯度: 99.84%

    Olmutinib (HM61713; BI-1482694) 是口服有效的，不可逆的第三代 EGFR 酪氨酸激酶抑制剂，其与激酶结构域附近的半胱氨酸残基结合。Olmutinib 可用于非小细胞肺癌的研究。

    Olmutinib(Synonyms: 奥莫替尼; HM61713, BI 1482694)

    Olmutinib Chemical Structure

    CAS No. : 1353550-13-6

    规格 价格 是否有货 数量
    Free Sample (0.1-0.5 mg)   Apply now  
    10 mM * 1 mL in DMSO ￥770 In-stock
    5 mg ￥700 In-stock
    10 mg ￥1200 In-stock
    50 mg ￥3800 In-stock
    100 mg ￥5200 In-stock
    200 mg ￥8200 In-stock
    500 mg   询价  
    1 g   询价  

    * Please select Quantity before adding items.

    Olmutinib 相关产品

    •相关化合物库:

    • Covalent Screening Library Plus
    • Drug Repurposing Compound Library Plus
    • FDA-Approved Drug Library Plus
    • Bioactive Compound Library Plus
    • Immunology/Inflammation Compound Library
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    • Protein Tyrosine Kinase Compound Library
    • FDA-Approved Drug Library
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    • Anti-Colorectal Cancer Compound Library

    生物活性

    Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC[1][2].

    IC50 & Target[1]

    EGFRExon 19 deletion

    9.2 nM (IC50, Cell Assay)

    EGFRL858R/T790M

    10 nM (IC50, Cell Assay)

    体外研究
    (In Vitro)

    Olmutinib potently inhibits EGFR in HCC827 cells expressing EGFRDEL19 (IC50=9.2 nM) and H1975 cells expressing EGFRL858R/T790M (IC50=10 nM). In contrast, the IC50 of olmutinib against cells expressing EGFRWT is 2225 nM[1].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial

    分子量

    486.59

    Formula

    C26H26N6O2S
    CAS 号

    1353550-13-6
    中文名称

    奥莫替尼
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : ≥ 44 mg/mL (90.43 mM)

    * “≥” means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.0551 mL 10.2756 mL 20.5512 mL
    5 mM 0.4110 mL 2.0551 mL 4.1102 mL
    10 mM 0.2055 mL 1.0276 mL 2.0551 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (4.27 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (4.27 mM，饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (4.27 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (4.27 mM，饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
    • 3.

      请依序添加每种溶剂： 10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.27 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (4.27 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献

    • [1]. Kim ES, et al. Olmutinib: First Global Approval. Drugs. 2016 Jul;76(11):1153-7.

      [2]. Mohamed W. Attwa, et al. Detection and characterization of olmutinib reactive metabolites by LC‐MS/MS: Elucidation of bioactivation pathways. Journal of Separation science. 18 November 2019.

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