标签归档：gska

GSK126(Synonyms: GSK2816126A)

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。

GSK126 (Synonyms: GSK2816126A) 纯度: 99.98%

GSK126 (GSK2816126A) 是一种有效，选择性的 EZH2 甲基转移酶抑制剂，IC50 为 9.9 nM。

GSK126(Synonyms: GSK2816126A)

GSK126 Chemical Structure

CAS No. : 1346574-57-9

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 ￥905 In-stock
5 mg ￥781 In-stock
10 mg ￥1162 In-stock
50 mg ￥2900 In-stock
100 mg ￥4000 In-stock
200 mg ￥7000 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

GSK126 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

GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM[1].

IC50 & Target[1]

EZH2

9.9 nM (IC50)

体外研究
(In Vitro)

GSK126 potently inhibits both wild-type and mutant EZH2 methyltransferase activity with similar potencies (Ki=0.5-3 nM) independent of substrate used, and is competitive with S-adenosyl-methionine (SAM) and non-competitive with peptide substrates. GSK126 is highly selective against other methyltransferases and multiple other protein classes (EZH1, IC50=680 nM)[1]. Treatment of three SCLC cell lines with GSK126, induces growth inhibition. SCLC cell lines (Lu130, H209, and DMS53) are treated with 0.5, 2, and 8 μM GSK126, and growth curve is analyzed by WST-8 assay. Inhibition of cellular growth by GSK126 treatment is observed at 8 μM in all the three cell lines, while Lu130 and H209 are more sensitive to GSK126, even at lower doses[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.
体内研究
(In Vivo)

GSK126 is administered intraperitoneally at a dose volume of 0.2 mL per 20 g body weight in female beige SCID mice. GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice[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

526.67

Formula

C31H38N6O2
CAS 号

1346574-57-9
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 : 12.5 mg/mL (23.73 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8987 mL 9.4936 mL 18.9872 mL
5 mM 0.3797 mL 1.8987 mL 3.7974 mL
10 mM 0.1899 mL 0.9494 mL 1.8987 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： 20% SBE-β-CD adjusted to pH 4-4.5 with 1 N acetic

    Solubility: 20 mg/mL (37.97 mM); Clear solution; Need ultrasonic and warming

  • 2.

    请依序添加每种溶剂： 50% PEG300    50% saline

    Solubility: 10 mg/mL (18.99 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 1.25 mg/mL (2.37 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.37 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.5 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

  • 4.

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

    Solubility: 1.25 mg/mL (2.37 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.25 mg/mL (2.37 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 12.5 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
  • 5.

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

    Solubility: ≥ 1.25 mg/mL (2.37 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.37 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 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 6.

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 0.82 mg/mL (1.56 mM); Clear solution

  • 7.

    请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.82 mg/mL (1.56 mM); Clear solution

*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]. McCabe MT, et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature. 2012 Dec 6;492(7427):108-12.

    [2]. Sato T, et al. PRC2 overexpression and PRC2-target gene repression relating to poorer prognosis in small cell lung cancer. Sci Rep. 2013 May 29;3:1911.
Kinase Assay
[1]

The five-member PRC2 complex (Flag-EZH2, EED, SUZ12, AEBP2, RbAp48) containing either wild-type or mutant (A677G, Y641N, Y641C, Y641H, Y641S or Y641F) EZH2 is prepared. GSK126 is dissolved in DMSO and tested at concentrations of 0.6 nM to 300 nM with a final DMSO concentration of 2.5%. In contrast to wild-type EZH2 which prefers H3K27me0 as a substrate in vitro, EZH2 Y641 mutants prefer H3K27me2 and have little activity with H3K27me0 or H3K27me1. The A677G mutant is distinct from both the wild-type and Y641 mutant forms of EZH2 in that it efficiently methylates H3K27me0, H3K27me1, and H3K27me2; therefore, histone H3 peptides (residues 21-44; 10 μM final) with either K27me0 (wild type, A677G EZH2), K27me1 (A677G EZH2), or K27me2 (A677G, Y641N, Y641C, Y641H, Y641S and Y641F EZH2) are used as methyltransferase substrates. GSK126 is added to plates followed by addition of 6 nM EZH2 complex and peptide. As the potency of GSK126 is at or near the tight binding limit of an assay run at [SAM]=Km, IC50 values are measured at a high concentration of the competitive substrate SAM relative to its Km (7.5 μM SAM where the SAM Km is 0.3 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.
Cell Assay
[2]

JUB– and PTRF-introduced DMS53 cells are seeded at density of 1×103 cells/well in 96-well plate, and cellular growth is analyzed using WST-8 kit at 12, 36, 60, and 84 h. Cellular growth of Lu130, H209, and DMS53 with treatment by DZNep or GSK126 is also analyzed using WST-8 kit. DZNep is dissolved in PBS at 5 mM, and cells are cultured at the final concentration of 5 μM. GSK126 is dissolved in DMSO at 10 mM, and cells are cultured at 0.5, 2, and 8 μM[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.
Animal Administration
[1]

Mice[1]
GSK126 or vehicle is administered intraperitoneally at a dose volume of 0.2 mL per 20 g body weight. Pfeiffer or KARPAS-422 cells (1×107) in 100% Matrigel are implanted subcutaneously in female beige SCID mice. Tumors are measured with calipers, and block randomized according to tumour size into treatment groups. For efficacy studies, 10 mice are randomized in each treatment group before the initiation of dosing and GSK126 treatment is initiated once the tumour volumes are approximately 200 mm3 in the Pfeiffer and KARPAS-422 studies and 500 mm3 in the KARPAS-422 intermittent dosing study. Mice are weighed and tumors measured with calipers twice weekly. Two-tailed t-tests are conducted assuming two samples of equal variance.

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]. McCabe MT, et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature. 2012 Dec 6;492(7427):108-12.

    [2]. Sato T, et al. PRC2 overexpression and PRC2-target gene repression relating to poorer prognosis in small cell lung cancer. Sci Rep. 2013 May 29;3:1911.

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Dabrafenib(Synonyms: 达拉非尼; GSK2118436A; GSK2118436)

发表于由

Dabrafenib (Synonyms: 达拉非尼; GSK2118436A; GSK2118436) 纯度: 99.97%

Dabrafenib (GSK2118436A) 是ATP竞争型的 Raf 抑制剂，抑制 C-Raf 和 B-RafV600E 的 IC50 分别为 5 nM 和 0.6 nM。

Dabrafenib(Synonyms: 达拉非尼; GSK2118436A; GSK2118436)

Dabrafenib Chemical Structure

CAS No. : 1195765-45-7

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 ￥743 In-stock
5 mg ￥650 In-stock
10 mg ￥850 In-stock
50 mg ￥1900 In-stock
100 mg ￥2900 In-stock
200 mg ￥4900 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Dabrafenib 相关产品

•相关化合物库:

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  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • MAPK Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library
  • Orally Active Compound Library
  • Glutamine Metabolism Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Targeted Therapy Drug Library
  • Anti-Liver Cancer Compound Library
  • Rare Diseases Drug Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively[4].

IC50 & Target[4]

BRafV600E

0.6 nM (IC50)

CRAF

5 nM (IC50)

体外研究
(In Vitro)

Dabrafenib (GSK2118436, 1 μM) with 0.01 μM GSK1120212 inhibits more than 90% of cell growth in the NRAS mutant clones. GSK2118436 is sufficient to reduce S6P phosphorylation in A375[1]. Dabrafenib suppresses the PolyP-mediated vascular barrier permeability, upregulation of inflammatory biomarkers, adhesion/migration of leukocytes, and activation and/or production of nuclear factor-κB, tumor necrosis factor-α, and interleukin-6[2]. Dabrafenib inhibits the release of HMGB1 and downregulates HMGB1-dependent inflammatory responses by enhancing the expressions of cell adhesion molecules (CAMs) in human endothelial cells[3].

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

Dabrafenib-treated females have mostly immature reproductive tracts with no evidence of ovulation, similar to age-matched controls; however, DAB-treated females have keratinized and histologically open vaginas[5].

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

分子量

519.56

Formula

C23H20F3N5O2S2
CAS 号

1195765-45-7
中文名称

达拉非尼
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 : ≥ 33 mg/mL (63.52 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 1.9247 mL 9.6235 mL 19.2471 mL
5 mM 0.3849 mL 1.9247 mL 3.8494 mL
10 mM 0.1925 mL 0.9624 mL 1.9247 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： 30% PEG400  0.5% Tween80  5% Propanediol  64.5%H2O

    Solubility: 5 mg/mL (9.62 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 0.5%HPMC

    Solubility: 2.5 mg/mL (4.81 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.81 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

  • 4.

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

    Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.81 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
  • 5.

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

    Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.81 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。

  • 6.

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: 2.5 mg/mL (4.81 mM); Suspended solution; Need ultrasonic

  • 7.

    请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther, 2012, 11(4), 909-920.

    [2]. Lee S, et al. Anti-inflammatory effects of dabrafenib on polyphosphate-mediated vascular disruption. Chem Biol Interact. 2016 Jul 22.

    [3]. Jung B, et al. Anti-septic effects of dabrafenib on HMGB1-mediated inflammatory responses. BMB Rep. 2016 Apr;49(4):214-9.

    [4]. Alexander M Menzies, et al. Dabrafenib and its potential for the treatment of metastatic melanoma. Drug Des Devel Ther. 2012; 6: 391–405.

    [5]. Posobiec LM, et al. Early Vaginal Opening in Juvenile Female Rats Given BRAF-Inhibitor Dabrafenib Is Not Associated with Early Physiologic Sexual Maturation. Birth Defects Res B Dev Reprod Toxicol. 2015 Dec;104(6):244-52.
Cell Assay
[1]

For longer term proliferation assays, cells are plated and treated with compound or combination of compounds in RMPI-1640 containing 10% FBS for 12 days. Compound treatments are replaced at least once during the assay. After 12 days, cells are stained with 0.5% methylene blue in 50% ethanol. Images are captured using flatbed scanner.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[5]

The rat pups selected as the test system are derived from 26 10-week-old, time-mated, virus-antibody-free SD (Crl:CD[SD]) female rats. Mated females are observed for natural deliveries from Day 20 to 23 pc (day parturition completed is designated PND 0). Litter examinations are conducted when parturition is complete, on PNDs 3 and 6, and included gender identification, individual pup weights, and external morphologic examinations. Parturient dams and their litters are selected for study based on clinical signs and body weights, and selected dams and their litters are randomized into study groups based on clinical observations and PND 3 litter mean body weights. On PND 3 or 4, litters are culled to four males and five females, with minimal fostering only when necessary to obtain the desired sex ratio, such that natural litters are maintained as much as possible. Records are kept of fostered pups of original and foster dams. All pups are identified by paw tattoo. To the extent possible, nonlittermates are assigned to subsets. DAB is formulated as a suspension in vehicle, 0.5% hydroxypropylmethylcellulose K15M, and 0.1% (v/v) Tween80 in purified water, and is given to juvenile male and female rats orally by gavage at a dose volume of 5 ml/kg, based on daily body weight.

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

  • [1]. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther, 2012, 11(4), 909-920.

    [2]. Lee S, et al. Anti-inflammatory effects of dabrafenib on polyphosphate-mediated vascular disruption. Chem Biol Interact. 2016 Jul 22.

    [3]. Jung B, et al. Anti-septic effects of dabrafenib on HMGB1-mediated inflammatory responses. BMB Rep. 2016 Apr;49(4):214-9.

    [4]. Alexander M Menzies, et al. Dabrafenib and its potential for the treatment of metastatic melanoma. Drug Des Devel Ther. 2012; 6: 391–405.

    [5]. Posobiec LM, et al. Early Vaginal Opening in Juvenile Female Rats Given BRAF-Inhibitor Dabrafenib Is Not Associated with Early Physiologic Sexual Maturation. Birth Defects Res B Dev Reprod Toxicol. 2015 Dec;104(6):244-52.

GSK2837808A

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。

GSK2837808A  纯度: ≥99.0%

GSK2837808A 是有效和选择性的乳酸脱氢酶A (LDHA) 抑制剂，对 hLDHA 和 hLDHB的 IC50 值分别为 2.6 和 43 nM。

GSK2837808A

GSK2837808A Chemical Structure

CAS No. : 1445879-21-9

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 ￥3001 In-stock
2 mg ￥1100 In-stock
5 mg ￥2100 In-stock
10 mg ￥3500 In-stock
25 mg ￥7200 In-stock
50 mg ￥11500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

GSK2837808A 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Glycolysis Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Glucose Metabolism Compound Library

生物活性

GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC50s of 2.6 and 43 nM for hLDHA and hLDHB, respectively.

IC50 & Target

IC50: 2.6 nM (hLDHA), 43 nM (hLDHB)[1]
体外研究
(In Vitro)

GSK2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. The potency of GSK2837808A across 30 cancer cell lines with different LDHA and LDHB expression levels ranges from 400 nM to no effect (EC50 reported as 30 μM). GSK2837808A potency does not correlate with LDHA, LDHB, or the total LDH expression levels. GSK2837808A inhibits lactate production in hypoxia but at higher concentrations than in normoxia (EC50=10 μM). It also reduces ECAR with EC50=10 μM. LDH inhibition by GSK2837808A alters multiple metabolic pathways in Snu398 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.
体内研究
(In Vivo)

Clearance following IV infusion of GSK2837808A at 0.25 mg/kg is shown to be 69 mL/minute/kg in rats, which exceeds the animal liver blood flow. Oral dosing of GSK2837808A at 50 mg/kg in rats or 100 mg/kg in mice results in blood compound levels at or below the detection limit of 2.5 ng/mL[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

649.62

Formula

C31H25F2N5O7S
CAS 号

1445879-21-9
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 (76.97 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5394 mL 7.6968 mL 15.3936 mL
5 mM 0.3079 mL 1.5394 mL 3.0787 mL
10 mM 0.1539 mL 0.7697 mL 1.5394 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 (3.85 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.85 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

*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]. Billiard J, et al. Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 2013 Sep 6;1(1):19.
Cell Assay
[1]

Sixty thousand Snu398 cells per well are plated in 6-well tissue culture plates in RPMI-1640 medium supplemented with 2.5% charcoal-stripped FBS. Cells are allowed to attach overnight and then DMSO control or the indicated doses of LDHA inhibitor dissolved in DMSO are added directly to the wells. After 4 to 8 days of incubation in the indicated oxygen conditions, adherent cells are trypsinized, counted, and had their viability assessed by the trypan-blue exclusion method using the Vi-Cell XR Cell Viability Analyzer[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 Administration
[1]

Mice: GSK2837808A is administered to male CD mice or male Sprague-Dawley rats orally or by intravenous (IV) infusion over 120 minutes into a femoral vein. Arterial blood samples are collected over time and GSK2837808A concentration is determined by liquid chromatography (LC)/MS/MS analysis[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]. Billiard J, et al. Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 2013 Sep 6;1(1):19.

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

GSK1838705A

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。

GSK1838705A  纯度: 99.28%

GSK1838705A是高效，可逆的 IGF-IR 和胰岛素受体 (insulin receptor) 抑制剂，IC50 值分别为2.0 和 1.6 nM。也可抑制 ALK，IC50 值为0.5 nM。

GSK1838705A

GSK1838705A Chemical Structure

CAS No. : 1116235-97-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1054 In-stock
5 mg ￥900 In-stock
10 mg ￥1600 In-stock
50 mg ￥6200 In-stock
100 mg ￥9500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

GSK1838705A 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Differentiation Inducing Compound Library
  • Endocrinology Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Angiogenesis Related Compound Library

生物活性

GSK1838705A is a potent and reversible IGF-IR and the insulin receptor inhibitor with IC50s of 2.0 and 1.6 nM, respectively. It also inhibits ALK with an IC50 of 0.5 nM.

IC50 & Target

IC50: 2.0 nM (IGF-IR), 1.6 nM (insulin receptor), 0.5 nM (ALK)[1]
体外研究
(In Vitro)

In cellular phosphorylation assays, GSK1838705A potently inhibits IGF-IR and insulin receptor phosphorylation with IC50s of 85 and 79 nM, respectively. appKi values are 0.7 nM for IGF-IR and 1.1 nM for insulin receptor using the filter binding assay. GSK1838705A inhibits the proliferation in a panel of cell lines derived from solid and hematologic tumors. The EC50s of GSK1838705A range from 20 nM to >8 μM, but are <1 μm in most multiple myeloma and ewing's sarcoma cell lines[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)

GSK1838705A shows robust antitumor activity in animal xenograft models. Tumor types likely to respond to GSK1838705A include multiple myeloma and Ewing’s sarcoma, as well as ALK-driven tumors (e.g., ALCL, NSCLC, and neuroblastoma). A single oral dose of GSK1838705A at 0.1 and 0.3 mg/kg results in 35% and 65% inhibition of IGF-IR phosphorylation, respectively, whereas doses ≥1 mg/kg results in complete inhibition of ligand-induced IGF-IR phosphorylation[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

532.57

Formula

C27H29FN8O3
CAS 号

1116235-97-2
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 : ≥ 100 mg/mL (187.77 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 1.8777 mL 9.3884 mL 18.7769 mL
5 mM 0.3755 mL 1.8777 mL 3.7554 mL
10 mM 0.1878 mL 0.9388 mL 1.8777 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: 3 mg/mL (5.63 mM); Suspended solution; Need ultrasonic

    此方案可获得 3 mg/mL (5.63 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 30.0 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

*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]. Sabbatini P, et al. GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol Cancer Ther. 2009 Oct;8(10):2811-20.
Kinase Assay
[1]

Baculovirus-expressed glutathione S-transferase–tagged proteins encoding the intracellular domain of IGF-IR (amino acids 957–1367) and IR (amino acids 979–1382) are used for determinations of IC50s by a homogeneous time-resolved fluorescence assay. A filter binding assay is used for appKi determinations using activated IGF-IR and IR kinases. Expanded kinase-selectivity profiling of GSK1838705A is carried out by screening the compound in the KinaseProfiler panel[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 seeded in 96-well dishes, incubated overnight at 37°C, and treated with DMSO or GSK1838705A for 72 h. For the NIH-3T3/LISN proliferation assays, cells are seeded on collagen-coated 96-well tissue culture plates and allowed to adhere for 24 h. The medium is replaced with serum-free medium and the cells are treated with GSK1838705A for 2 h. Cells are incubated for 72 h after addition of IGF-I (30 ng/mL). Cell proliferation is quantified using the CellTiter-Glo Luminescent Cell Viability Assay. IC50s are determined from cytotoxicity curves using a four-parameter curve fit software package[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 Administration
[1]

Mice: Exponentially growing cells are implanted s.c. into the right flank of 8- to 12-wk-old female nu/nu CD-1 or SCID mice. Mice are dosed p.o. with the formulating vehicle or GSK1838705A. Mice are weighed and tumors measured by calipers twice weekly. Tumor volumes are calculated[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]. Sabbatini P, et al. GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol Cancer Ther. 2009 Oct;8(10):2811-20.

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

GSK1324726A(Synonyms: I-BET726)

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。

GSK1324726A (Synonyms: I-BET726) 纯度: 98.0%

GSK1324726A 是一种有效的选择性 BET 蛋白抑制剂，高亲和力结合到 BRD2 (IC50=41 nM)，BRD3 (IC50=31 nM) 和 BRD4 (IC50=22 nM)。

GSK1324726A(Synonyms: I-BET726)

GSK1324726A Chemical Structure

CAS No. : 1300031-52-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1270 In-stock
5 mg ￥1150 In-stock
10 mg ￥2000 In-stock
50 mg ￥5700 In-stock
100 mg ￥9300 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

GSK1324726A 相关产品

•相关化合物库:

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

生物活性

GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).

IC50 & Target

IC50: 22 nM (BRD4), 31 nM (BRD3), 41 nM (BRD2)[1]
体外研究
(In Vitro)

A panel of neuroblastoma cell lines are treated with GSK1324726A (I-BET726), and observed potent growth inhibition and cytotoxicity in most cell lines irrespective of MYCN copy number or expression level. All neuroblastoma cell lines tested exhibit potent growth inhibition, with a median growth IC50 value (gIC50; inhibitor concentration resulting in 50% growth inhibition) equal to 75 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.
体内研究
(In Vivo)

GSK1324726A (I-BET726) inhibits neuroblastoma tumor growth. In the SK-N-AS model, mice in the vehicle group are euthanized on day 14 due to large tumor size. While there is no significant difference in tumor growth between the vehicle and GSK1324726A (5 mg/kg) group, 58% tumor growth inhibition (TGI) is observed in the GSK1324726A (15 mg/kg) group on day 14 of the study (n=9; p=0.006). Mice in the GSK1324726A (15 mg/kg) group are treated for an additional 7 days before tumor volume reaches a level comparable to that observed in the vehicle group, at which point the study is terminated. Tumors in the CHP-212 model grow much more slowly. After 42 days, tumors in vehicle-treated mice are only half the size those in the SK-N-AS model at the end of the study (Day 14). In the CHP-212 model, treatment with 5 mg/kg GSK1324726A results in TGI equal to 50% (n=8; p=0.1816), and mice in the 15 mg/kg group exhibits a TGI of 82% at the end of the study (n=5; p=0.0488)[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

434.91

Formula

C25H23ClN2O3
CAS 号

1300031-52-0
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 : ≥ 46 mg/mL (105.77 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 2.2993 mL 11.4966 mL 22.9933 mL
5 mM 0.4599 mL 2.2993 mL 4.5987 mL
10 mM 0.2299 mL 1.1497 mL 2.2993 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 (5.75 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.75 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% corn oil

    Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.75 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]. Wyce A, et al. BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models. PLoS One. 2013 Aug 23;8(8):e72967.

    [2]. Gosmini R, et al. The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem. 2014 Oct 9;57(19):8111-31.
Cell Assay
[1]

Cell line growth-death assays are performed with a few modifications. Briefly, cells are seeded into 384-well or 96-well plates at a density optimized for 6 days of growth. The following day, T0 measurements are taken using CellTiter-Glo, CellTiter-Fluor, or CyQuant Direct. Plates are read on an Envision, Safire 2, or SpectraMax Gemini EM plate reader. Remaining plates are treated with DMSO or a titration of GSK1324726A. Cells are incubated for 6 days and developed. Results are plotted as a percentage of the T0 value, normalized to 100%, versus concentration of compound. A 4-parameter equation is used to generate concentration response curves. Growth IC50 (gIC50) values are calculated at the mid-point of the growth window (between DMSO and T0 values). Ymin-T0 values are calculated by subtracting the T0 value (100%) from the Ymin value on the curve, and are a measure of net population cell growth or death[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 Administration
[1][2]

Mice[1]
CHP-212 (1×107) or SK-N-AS (5×106) cells in 100% matrigel are implanted subcutaneously into the right flank of approximately 9 week old female nude (Crl:CD-1-Foxn1 nu) mice. Tumors are measured with calipers and randomized using stratified sampling according to tumor size into treatment groups of 10 mice. GSK1324726A in vehicle or vehicle alone is administered orally by individual body weight at 10mls/kg. Mice are weighed and tumors are measured with calipers twice weekly, and mice are observed daily for any adverse treatment affects. Mice are euthanized using CO2 inhalation according to AVMA guidelines after two consecutive tumor measurements greater than 2500mm3, or if body weight loss greater than 20% is observed. For mouse pharmacodynamic studies, mice are euthanized as described above. Tumors are harvested from euthanized mice and placed in RNAlater for RNA isolation. Blood is collected after euthanasia via cardiac puncture.
Rats[2]
Male CD rats (253-283 g) are surgically prepared with implanted cannulae in the femoral vein (for GSK1324726A administration) and jugular vein (for blood sampling). Each rat receives Duphacillin (100 mg/kg s.c.) and Carprofen (7.5 mg/kg s.c.) as a pre-operative antibiotic and analgesic respectively. Each rat is allowed to recover for at least 2 days prior to dosing. Rats have free access to food and water throughout. Rat PK studies are conducted as a crossover design over 2 dosing occasions, with 3 days between dose administrations. Serial blood samples are taken (via indwelling jugular cannula) up to 26 h post dose administration on both dosing occasions. On study day 1, n=3 male rats each receives a 1 h intravenous infusion of GSK1324726A formulated in DMSO and 10% (w/v) KleptoseTM in saline (2%:98%) at a concentration of 0.2 mg/mL and the dose is filtered using a ca. 0.2 μm syringe filter unit. GSK1324726A is administered as a 1 h i.v. infusion at 5 mL/kg/h to achieve a target dose of 1 mg/kg. On study day 2, the same three rats each receives an oral administration of GSK1324726A suspended in 3% Pharmacoat 603/0.2% Sodium Lauryl Sulphate (w/v) aq. at a concentration of 0.6 mg/mL administered by gavage at 5 mL/kg to achieve a target dose of 3 mg/kg. At the end of the study the rats are euthanised by administration of sodium pentobarbital through the jugular vein cannula.

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]. Wyce A, et al. BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models. PLoS One. 2013 Aug 23;8(8):e72967.

    [2]. Gosmini R, et al. The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem. 2014 Oct 9;57(19):8111-31.

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

I-BET151(Synonyms: GSK1210151A)

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。

I-BET151 (Synonyms: GSK1210151A) 纯度: 99.81%

I-BET151 (GSK1210151A) 是一种 BET 溴结构域 (BET bromodomain) 抑制剂，抑制 BRD4，BRD2 和 BRD3 的 pIC50 分别为 6.1，6.3 和 6.6。

I-BET151(Synonyms: GSK1210151A)

I-BET151 Chemical Structure

CAS No. : 1300031-49-5

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 ￥1377 In-stock
5 mg ￥1252 In-stock
10 mg ￥1989 In-stock
50 mg ￥6412 In-stock
100 mg ￥9360 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

I-BET151 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

生物活性

I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively[1][2].

IC50 & Target

pIC50: 6.1 (BRD4), 6.3 (BRD2), 6.6 (BRD3)[1]
体外研究
(In Vitro)

I-BET151 (1 μM; 72 hours) treatment displays the majority of live cells resided in the G0 phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation[2].
I-BET151 (100 nM; 72 hours) causes a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2 phase[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.

Cell Viability Assay[2]

Cell Line: H929 cells
Concentration: 1 μM
Incubation Time: 72 hours
Result: Displays the majority of live cells resided in the G0 phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation.

Cell Proliferation Assay[2]

Cell Line: H929 cells
Concentration: 100 nM
Incubation Time: 72 hours
Result: Caused a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2 phase.

体内研究
(In Vivo)

I-BET151 demonstrates low blood clearance in the rat (~20% liver blood flow) and good oral systemic exposure which resulted in good oral bioavailability. High clearance is observed in the dog (~95% liver blood flow). The systemic exposure in the dog is low, resulting in a poor oral bioavailability of 16%. The high blood clearance in dog correlates well with the high intrinsic clearance observed in dog microsomes and hepatocytes, whereas the low intrinsic clearances seen in rat and mouse (mouse IVC 1.6 mL/min/g; CLb 8 mL/min/kg) correlate with lower in vivo blood clearances in these species. Due to the low systemic exposure observed in the dog, I-BET151 is investigated in the mini-pig as a potential second species for toxicological evaluation where it showed low clearance (~32% liver blood flow) and good bioavailability (65%)[1].
I-BET151 (30 mg/kg; i.p.; daily for 21 days)-treats mice has four- to five fold smaller myeloma tumors and a significantly reduces rate of tumor size doubling than vehicle-treated mice[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.

Animal Model: Mice (model of subcutaneous myeloma)[2]
Dosage: 50 mg/kg
Administration: I.p.; daily for 21 days
Result: Reduced rate of tumor size doubling than vehicle-treated mice.

分子量

415.44

Formula

C23H21N5O3
CAS 号

1300031-49-5
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 (240.71 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 2.4071 mL 12.0354 mL 24.0709 mL
5 mM 0.4814 mL 2.4071 mL 4.8142 mL
10 mM 0.2407 mL 1.2035 mL 2.4071 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 (6.02 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.02 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 (6.02 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.02 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 (6.02 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.02 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： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

  • 5.

    请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

  • 6.

    请依序添加每种溶剂： 1% DMSO    99% saline

    Solubility: 0.5 mg/mL (1.20 mM); Suspended solution; Need ultrasonic

*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]. Seal J, et al. Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A). Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72.

    [2]. Chaidos A, et al. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood. 2014 Jan 30;123(5):697-705.

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

GSK429286A

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。

GSK429286A  纯度: 98.75%

GSK429286A是选择性的 ROCK1 抑制剂，IC50 值为14 nM。

GSK429286A

GSK429286A Chemical Structure

CAS No. : 864082-47-3

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 ￥720 In-stock
5 mg ￥650 In-stock
10 mg ￥1000 In-stock
50 mg ￥2600 In-stock
100 mg ￥4500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

GSK429286A 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Stem Cell Signaling Compound Library
  • TGF-beta/Smad Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Cytoskeleton Compound Library
  • Targeted Diversity Library

生物活性

GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.

IC50 & Target[1]

ROCK1

14 nM (IC50)

RSK

780 nM (IC50)

p70S6K

1940 nM (IC50)

体外研究
(In Vitro)

GSK429286A at 1 μM reduces ROCK2 activity over 20-fold, under conditions in which the only other kinase tested that is significantly inhibited is MSK1 whose activity is reduced ~5-fold. GSK429286A is a more selective ROCK2 inhibitor than the widely utilized ROCK inhibitor Y-27632 as assessed on kinase-specificity panel, and does not significantly inhibit LRRK2 even at doses as high as 30 μM (500-fold higher than IC50 of inhibition of ROCK2). GSK429286A slightly inhibits RSK and p70S6K with IC50 of 0.78 μM and 1.94 μM, respectively. GSK429286A significantly inhibits rat aortic ring dilation with IC50 of 190 nM[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.
体内研究
(In Vivo)

GSK429286A has 61% oral bioavailability in male Sprague-Dawley rats. Oral administration of GSK429286A at single doses of 3-30 mg/kg dramatically reduces mean arterial pressure in the spontaneously hypertensive rats (SHRs) in a dose-dependent manner, with a maximum decrease of 50 mmHg after approximately 2 hours treatment at dose of 30 mg/kg[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

432.37

Formula

C21H16F4N4O2
CAS 号

864082-47-3
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 : ≥ 51 mg/mL (117.95 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 2.3128 mL 11.5642 mL 23.1283 mL
5 mM 0.4626 mL 2.3128 mL 4.6257 mL
10 mM 0.2313 mL 1.1564 mL 2.3128 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 (4.81 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.81 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 (4.81 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.81 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 (4.81 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.81 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]. Goodman KB et al Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J Med Chem. 2007 Jan 11;50(1):6-9.

    [2]. Nichols RJ et al Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson’s disease. Biochem J. 2009 Oct 23;424(1):47-60.
Animal Administration
[1]

Rats: Spontaneously hypertensive rats (SHRs) are treated with GSK429286A to establish its effect on mean arterial pressure. Compound is administered by single dose oral gavage (3, 10, 30 mg/kg)[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]. Goodman KB et al Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J Med Chem. 2007 Jan 11;50(1):6-9.

    [2]. Nichols RJ et al Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson’s disease. Biochem J. 2009 Oct 23;424(1):47-60.

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

GSK2643943A

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。

GSK2643943A  纯度: 98.28%

GSK2643943A 是一种去泛素化酶 (DUB) 的抑制剂，其对 USP20/Ub-Rho 的 IC50 值为 160 nM。

GSK2643943A

GSK2643943A Chemical Structure

CAS No. : 2449301-27-1

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 ￥2200 In-stock
5 mg ￥2000 In-stock
10 mg ￥3300 In-stock
25 mg ￥7000 In-stock
50 mg ￥11000 In-stock
100 mg ￥19000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

GSK2643943A 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Ubiquitination Compound Library

生物活性

GSK2643943A is a deubiquitylating enzyme (DUB) inhibitor, with an IC50 of 160 nM for USP20/Ub-Rho.

IC50 & Target

IC50: 160 nM (USP20/Ub-Rho)[1][2].
分子量

277.30

Formula

C17H12FN3
CAS 号

2449301-27-1
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 : ≥ 125 mg/mL (450.78 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 3.6062 mL 18.0310 mL 36.0620 mL
5 mM 0.7212 mL 3.6062 mL 7.2124 mL
10 mM 0.3606 mL 1.8031 mL 3.6062 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 (7.50 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.50 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 (7.50 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (7.50 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 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
*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]. Harrigan JA, et al.Deubiquitylating enzymes and drug discovery: emerging opportunities.Nat Rev Drug Discov. 2018 Jan;17(1):57-78.

    [2]. Nishi Kumari, et al. Targeting the Ubiquitin Proteasome System in Cancer. Neoplasm. 2017 Dec.

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GSK1904529A

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。

GSK1904529A  纯度: 99.22%

GSK1904529A 是一种有效的，选择性的，具有口服活性和 ATP 竞争性的胰岛素样生长因子 1 受体 (IGF-1R) 和胰岛素受体 (IR) 抑制剂，IC50 值分别为 27 和 25 nM。GSK1904529A 在其他 45 种丝氨酸/苏氨酸和酪氨酸激酶中显示出较弱的活性 (IC50>1 μM)。GSK1904529A 具有抗肿瘤活性。

GSK1904529A

GSK1904529A Chemical Structure

CAS No. : 1089283-49-7

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 ￥1270 In-stock
10 mg ￥1350 In-stock
50 mg ￥3450 In-stock
100 mg ￥6250 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

GSK1904529A 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Differentiation Inducing Compound Library
  • Diabetes Related Compound Library
  • Endocrinology Compound Library
  • Orally Active Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Angiogenesis Related Compound Library

生物活性

GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity[1][2].

IC50 & Target

IC50: 27 nM (IGF-1R), 25 nM (IR)[1]
体外研究
(In Vitro)

GSK1904529A displays high affinities for IGF-1R and IR, with Kis of 1.6 and 1.3 nM, respectively[1].
GSK1904529A (72 h) inhibits tumor cells proliferation with IC50s ranges from 35 nM to >30 μM, and Ewing’s sarcoma and multiple myeloma cell lines are greatest sensitive[1].
GSK1904529A (0.03-3 μM; 24 and 48 h) arrests cells at the G1 phase of the cell cycle[1].
GSK1904529A (2 h) inhibits phosphorylation of IGF-IR and IR with IC50s of 22 and 19 nM in NIH-3T3/LISN and NIH-3T3-hIR cells, respectively[1].
GSK1904529A (0.01-3 μM; 4 h) blocks the major downstream signal transduction pathways mediated by IGF-IR and IR in NIH-3T3/LISN and NIH-3T3-hIR 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: COLO 205, MCF-7, and NCI-H929 cells
Concentration: 0, 0.03, 0.1, 0.3, 1, 3 μM
Incubation Time: 24 and 48 hours
Result: Increased the accumulation in G1 and decreased accumulation in S and G2-M phases of the cell cycle.

Western Blot Analysis[1]

Cell Line: NIH-3T3/LISN and NIH-3T3-hIR cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 μM
Incubation Time: 4 hours
Result: Inhibited the ligand-induced phosphorylation of IGF-IR and IR at concentrations >0.01 μM.
Decreased the phosphorylation of AKT, IRS-1, and ERK.

体内研究
(In Vivo)

GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has antitumor activity in mice[1].
GSK1904529A (1-30 mg/kg; a single p.o.) decreases IGF-I-induced IGF-IR phosphorylation in a dose-dependent manner in mice[1].
GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has no significant alterations in the blood glucose levels in mice[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: Female athymic nu/nu CD-1 mice are bring NIH-3T3/LISN tumor[1]
Dosage: 30 mg/kg
Administration: P.o. once or twice daily for 21 d
Result: Resulted in 56% (once daily) and 98% (twice daily) inhibition of tumor growth.
No significant decrease in body weight on the once-daily schedule.
Observed 11-13% of body weight loss, and recovered to near baseline 6 days after the cessation of treatment in twice-daily group.

分子量

851.96

Formula

C44H47F2N9O5S
CAS 号

1089283-49-7
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 : 50 mg/mL (58.69 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1738 mL 5.8688 mL 11.7376 mL
5 mM 0.2348 mL 1.1738 mL 2.3475 mL
10 mM 0.1174 mL 0.5869 mL 1.1738 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: ≥ 2.75 mg/mL (3.23 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (3.23 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 27.5 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

*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]. Sabbatini P, et al. Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase. Clin Cancer Res, 2009, 15(9), 3058-3067.

    [2]. Zhou Q, et, al. GSK1904529A, an insulin-like growth factor-1 receptor inhibitor, inhibits glioma tumor growth, induces apoptosis and inhibits migration. Mol Med Rep. 2015 Sep;12(3):3381-3385.

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

I-BET151 dihydrochloride(Synonyms: GSK1210151A dihydrochloride)

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。

I-BET151 dihydrochloride (Synonyms: GSK1210151A dihydrochloride)

I-BET151 dihydrochloride (GSK1210151A dihydrochloride) 是一种 BET 溴结构域 (BET bromodomain) 抑制剂，抑制 BRD4，BRD2 和 BRD3 的 pIC50 分别为 6.1，6.3 和 6.6。

I-BET151 dihydrochloride(Synonyms: GSK1210151A dihydrochloride)

I-BET151 dihydrochloride Chemical Structure

CAS No. : 1883545-47-8

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

* Please select Quantity before adding items.

I-BET151 dihydrochloride 的其他形式现货产品:

I-BET151

生物活性

I-BET151 dihydrochloride (GSK1210151A dihydrochloride) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively[1][2].

IC50 & Target

pIC50: 6.1 (BRD4), 6.3 (BRD2), 6.6 (BRD3)[1]
体外研究
(In Vitro)

I-BET151 dihydrochloride (1 μM; 72 hours) treatment displays the majority of live cells resided in the G0 phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation[2].
I-BET151 dihydrochloride (100 nM; 72 hours) causes a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2 phase[2].

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

Cell Viability Assay[2]

Cell Line: H929 cells
Concentration: 1 μM
Incubation Time: 72 hours
Result: Displays the majority of live cells resided in the G0 phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation.

Cell Proliferation Assay[2]

Cell Line: H929 cells
Concentration: 100 nM
Incubation Time: 72 hours
Result: Caused a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2 phase.

体内研究
(In Vivo)

I-BET151 dihydrochloride demonstrates low blood clearance in the rat (~20% liver blood flow) and good oral systemic exposure which resulted in good oral bioavailability. High clearance is observed in the dog (~95% liver blood flow). The systemic exposure in the dog is low, resulting in a poor oral bioavailability of 16%. The high blood clearance in dog correlates well with the high intrinsic clearance observed in dog microsomes and hepatocytes, whereas the low intrinsic clearances seen in rat and mouse (mouse IVC 1.6 mL/min/g; CLb 8 mL/min/kg) correlate with lower in vivo blood clearances in these species. Due to the low systemic exposure observed in the dog, I-BET151 dihydrochloride is investigated in the mini-pig as a potential second species for toxicological evaluation where it showed low clearance (~32% liver blood flow) and good bioavailability (65%)[1].
I-BET151 dihydrochloride (30 mg/kg; i.p.; daily for 21 days)-treats mice has four- to five fold smaller myeloma tumors and a significantly reduces rate of tumor size doubling than vehicle-treated mice[2].

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

Animal Model: Mice (model of subcutaneous myeloma)[2]
Dosage: 50 mg/kg
Administration: I.p.; daily for 21 days
Result: Reduced rate of tumor size doubling than vehicle-treated mice.

分子量

488.37

Formula

C23H23Cl2N5O3
CAS 号

1883545-47-8
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]. Seal J, et al. Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A). Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72.

    [2]. Chaidos A, et al. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood. 2014 Jan 30;123(5):697-705.

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

Dabrafenib-d9(Synonyms: GSK2118436A-d9; GSK2118436-d9)

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。

Dabrafenib-d9 (Synonyms: GSK2118436A-d9; GSK2118436-d9)

Dabrafenib-d9 (GSK2118436A-d9) 是 Dabrafenib 的氘代物。Dabrafenib (GSK2118436A) 是ATP竞争型的 Raf 抑制剂，抑制 C-Raf 和 B-RafV600E 的 IC50 分别为 5 nM 和 0.6 nM。

Dabrafenib-d9(Synonyms: GSK2118436A-d9; GSK2118436-d9)

Dabrafenib-d9 Chemical Structure

CAS No. : 1423119-98-5

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

* Please select Quantity before adding items.

生物活性

Dabrafenib-d9 (GSK2118436A-d9) is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively[4].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

528.62

Formula

C23H11D9F3N5O2S2
CAS 号

1423119-98-5
中文名称

达拉非尼 d9
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther, 2012, 11(4), 909-920.

    [3]. Lee S, et al. Anti-inflammatory effects of dabrafenib on polyphosphate-mediated vascular disruption. Chem Biol Interact. 2016 Jul 22.

    [4]. Jung B, et al. Anti-septic effects of dabrafenib on HMGB1-mediated inflammatory responses. BMB Rep. 2016 Apr;49(4):214-9.

    [5]. Alexander M Menzies, et al. Dabrafenib and its potential for the treatment of metastatic melanoma. Drug Des Devel Ther. 2012; 6: 391–405.

    [6]. Posobiec LM, et al. Early Vaginal Opening in Juvenile Female Rats Given BRAF-Inhibitor Dabrafenib Is Not Associated with Early Physiologic Sexual Maturation. Birth Defects Res B Dev Reprod Toxicol. 2015 Dec;104(6):244-52.

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