MI-136

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。

MI-136  纯度: 98.64%

MI-136 是 menin-MLL (PPI) 蛋白互作的抑制剂,其 IC50 值为31 nM,Kd 值为23.6 nM。MI-136 可抑制 AR 信号通路,有用于去势抵抗性肿瘤的潜能。

MI-136

MI-136 Chemical Structure

CAS No. : 1628316-74-4

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 ¥1160 In-stock
5 mg ¥1050 In-stock
10 mg ¥1800 In-stock
50 mg ¥6500 In-stock
100 mg ¥11250 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MI-136 相关产品

相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library
  • Transcription Factor Targeted Library

生物活性

MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors[1][2].

体外研究
(In Vitro)

MI-136 (0-20) exhibits IC50values of 5.59 μM, 7.15 μM, 5.37 μM and 19.76 μM in LNCaP, VCaP, 22rv1 and PNT2 cells[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 Proliferation Assay[2]

Cell Line: AR positive cell lines such as VCaP, LNCaP and 22RV1.
Concentration: 0-20 μM.
Incubation Time: 24 h.
Result: Inhibited cell proliferation.

体内研究
(In Vivo)

MI-136 exhibits T1/2 of 3.1 h after po administration[1].
MI-136 (40 mg/kg, ip) leads to a significant decrease in the growth of castration-resistant VCaP tumors[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: VCaP xenografts[2].
Dosage: 40 mg/kg.
Administration: Intraperitoneal injection, 5 days a week.
Result: Led to a significant decrease in the growth of castration-resistant VCaP tumors compared to vehicle controls.

分子量

470.51

Formula

C23H21F3N6S

CAS 号

1628316-74-4

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 : 110 mg/mL (233.79 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1254 mL 10.6268 mL 21.2535 mL
5 mM 0.4251 mL 2.1254 mL 4.2507 mL
10 mM 0.2125 mL 1.0627 mL 2.1254 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 (5.84 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.84 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

  • 2.

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

    Solubility: ≥ 2.75 mg/mL (5.84 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.84 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 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: ≥ 2.75 mg/mL (5.84 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.84 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 27.5 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]. Dmitry Borkin, et al. Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL). J Med Chem. 2016 Feb 11;59(3):892-913.

    [2]. Rohit Malik, et al. Targeting the MLL complex in castration-resistant prostate cancer. Nat Med. 2015 Apr;21(4):344-52.

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

MI-192

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。

MI-192 

MI-192 是一种选择性 HDAC2HDAC3 抑制剂,IC50 分别为 30 nM 和 16 nM。MI-192 对 HDAC2/3 的选择性比其他 HDAC 异构体更高。MI-192 诱导髓系白血病细胞凋亡 (apoptosis)。抗癌和神经保护活性。

MI-192

MI-192 Chemical Structure

CAS No. : 1415340-63-4

规格 是否有货
1 mg 询价
5 mg 询价

* Please select Quantity before adding items.

生物活性

MI-192 is a selective HDAC2 and HDAC3 inhibitor with IC50s of 30 nM and 16 nM, respectively. MI-192 is more selective for HDAC2/3 than other HDAC isomers.MI-192 induces myeloid leukaemic cells apoptosis. Anticaner and neuroprotective activities[1][2].

体外研究
(In Vitro)

MI-192 (0.15-1 μM; 72 h) induces differentiation and is cytotoxic through promotion of apoptosis in acute myeloid leukaemic cell lines U937, HL60 and Kasumi-1[1].

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

Apoptosis Analysis[1]

Cell Line: HL60 and Kasumi-1 cells
Concentration: 150 nM, 300 nM, 500 nM, 1 μM
Incubation Time: 72 h
Result: Induced a substantial degree of apoptosis in both HL60 and Kasumi-1 cells.

体内研究
(In Vivo)

MI-192 (40 mg/kg; i.p; once a day; for 3 days) shows the neuroprotective activity in the mouse brain subjected to photothrombotic stroke[2].

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

Animal Model: Adult male outbred mice CD-1 (20-25 g) with photothrombotic stroke (PTS)[2]
Dosage: 40 mg/kg
Administration: i.p; once a day; for 3 days
Result: Reduced the volume of the PTS-induced infarction core in the mouse brain, partly restored the functional symmetry in the forelimb use, decreased the level of PTS-induced apoptosis and acetylation of α-tubulin characteristic for stable microtubules, and increased the expression of GAP-43 in the cerebral cortex of the damaged hemisphere.

分子量

383.44

Formula

C24H21N3O2

CAS 号

1415340-63-4

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]. Marjorie Boissinot, et al. Induction of differentiation and apoptosis in leukaemic cell lines by the novel benzamide family histone deacetylase 2 and 3 inhibitor MI-192. Leuk Res. 2012 Oct;36(10):1304-10.

    [2]. S V Demyanenko, et al. The Neuroprotective Effect of the HDAC2/3 Inhibitor MI192 on the Penumbra After Photothrombotic Stroke in the Mouse Brain. Mol Neurobiol. 2020 Jan;57(1):239-248.

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

MI-192

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。

MI-192 

MI-192 是一种选择性 HDAC2HDAC3 抑制剂,IC50 分别为 30 nM 和 16 nM。MI-192 对 HDAC2/3 的选择性比其他 HDAC 异构体更高。MI-192 诱导髓系白血病细胞凋亡 (apoptosis)。抗癌和神经保护活性。

MI-192

MI-192 Chemical Structure

CAS No. : 1415340-63-4

规格 是否有货
1 mg 询价
5 mg 询价

* Please select Quantity before adding items.

生物活性

MI-192 is a selective HDAC2 and HDAC3 inhibitor with IC50s of 30 nM and 16 nM, respectively. MI-192 is more selective for HDAC2/3 than other HDAC isomers.MI-192 induces myeloid leukaemic cells apoptosis. Anticaner and neuroprotective activities[1][2].

体外研究
(In Vitro)

MI-192 (0.15-1 μM; 72 h) induces differentiation and is cytotoxic through promotion of apoptosis in acute myeloid leukaemic cell lines U937, HL60 and Kasumi-1[1].

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

Apoptosis Analysis[1]

Cell Line: HL60 and Kasumi-1 cells
Concentration: 150 nM, 300 nM, 500 nM, 1 μM
Incubation Time: 72 h
Result: Induced a substantial degree of apoptosis in both HL60 and Kasumi-1 cells.

体内研究
(In Vivo)

MI-192 (40 mg/kg; i.p; once a day; for 3 days) shows the neuroprotective activity in the mouse brain subjected to photothrombotic stroke[2].

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

Animal Model: Adult male outbred mice CD-1 (20-25 g) with photothrombotic stroke (PTS)[2]
Dosage: 40 mg/kg
Administration: i.p; once a day; for 3 days
Result: Reduced the volume of the PTS-induced infarction core in the mouse brain, partly restored the functional symmetry in the forelimb use, decreased the level of PTS-induced apoptosis and acetylation of α-tubulin characteristic for stable microtubules, and increased the expression of GAP-43 in the cerebral cortex of the damaged hemisphere.

分子量

383.44

Formula

C24H21N3O2

CAS 号

1415340-63-4

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]. Marjorie Boissinot, et al. Induction of differentiation and apoptosis in leukaemic cell lines by the novel benzamide family histone deacetylase 2 and 3 inhibitor MI-192. Leuk Res. 2012 Oct;36(10):1304-10.

    [2]. S V Demyanenko, et al. The Neuroprotective Effect of the HDAC2/3 Inhibitor MI192 on the Penumbra After Photothrombotic Stroke in the Mouse Brain. Mol Neurobiol. 2020 Jan;57(1):239-248.

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

MI-192

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。

MI-192 

MI-192 是一种选择性 HDAC2HDAC3 抑制剂,IC50 分别为 30 nM 和 16 nM。MI-192 对 HDAC2/3 的选择性比其他 HDAC 异构体更高。MI-192 诱导髓系白血病细胞凋亡 (apoptosis)。抗癌和神经保护活性。

MI-192

MI-192 Chemical Structure

CAS No. : 1415340-63-4

规格 是否有货
1 mg 询价
5 mg 询价

* Please select Quantity before adding items.

生物活性

MI-192 is a selective HDAC2 and HDAC3 inhibitor with IC50s of 30 nM and 16 nM, respectively. MI-192 is more selective for HDAC2/3 than other HDAC isomers.MI-192 induces myeloid leukaemic cells apoptosis. Anticaner and neuroprotective activities[1][2].

体外研究
(In Vitro)

MI-192 (0.15-1 μM; 72 h) induces differentiation and is cytotoxic through promotion of apoptosis in acute myeloid leukaemic cell lines U937, HL60 and Kasumi-1[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.

Apoptosis Analysis[1]

Cell Line: HL60 and Kasumi-1 cells
Concentration: 150 nM, 300 nM, 500 nM, 1 μM
Incubation Time: 72 h
Result: Induced a substantial degree of apoptosis in both HL60 and Kasumi-1 cells.

体内研究
(In Vivo)

MI-192 (40 mg/kg; i.p; once a day; for 3 days) shows the neuroprotective activity in the mouse brain subjected to photothrombotic stroke[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: Adult male outbred mice CD-1 (20-25 g) with photothrombotic stroke (PTS)[2]
Dosage: 40 mg/kg
Administration: i.p; once a day; for 3 days
Result: Reduced the volume of the PTS-induced infarction core in the mouse brain, partly restored the functional symmetry in the forelimb use, decreased the level of PTS-induced apoptosis and acetylation of α-tubulin characteristic for stable microtubules, and increased the expression of GAP-43 in the cerebral cortex of the damaged hemisphere.

分子量

383.44

Formula

C24H21N3O2

CAS 号

1415340-63-4

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]. Marjorie Boissinot, et al. Induction of differentiation and apoptosis in leukaemic cell lines by the novel benzamide family histone deacetylase 2 and 3 inhibitor MI-192. Leuk Res. 2012 Oct;36(10):1304-10.

    [2]. S V Demyanenko, et al. The Neuroprotective Effect of the HDAC2/3 Inhibitor MI192 on the Penumbra After Photothrombotic Stroke in the Mouse Brain. Mol Neurobiol. 2020 Jan;57(1):239-248.

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

MI-2-2

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。

MI-2-2 

MI-2-2 是一种有效的 menin-MLL 抑制剂。MI-2-2 以低纳摩尔亲和力 (Kd=22 nM) 与 menin 结合,并非常有效地破坏 menin 和 MLL 之间的二价蛋白质-蛋白质相互作用。MI-2-2 在 MLL 白血病细胞中具有特异且非常显著的活性,包括抑制细胞增殖、下调 Hoxa9 表达和分化。

MI-2-2

MI-2-2 Chemical Structure

CAS No. : 1454920-20-7

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

MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation[1].

体外研究
(In Vitro)

MI-2-2 is capable of inhibiting both the interaction of menin with MBM1 (IC50= 46 nM) and with the bivalent fragment of MLL that comprises both MBM1 and MBM2 (IC50=520 nM). MI-2-2 exhibits very pronounced activities at low micromolar concentrations in BMCs transformed with MLL-AF9 and in MV4;11, a human leukemia cell line harboring the MLL-AF4 translocation[1].

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

分子量

415.50

Formula

C17H20F3N5S2

CAS 号

1454920-20-7

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]. Shi A, et al. Structural insights into inhibition of the bivalent menin-MLL interaction by small molecules in leukemia. Blood. 2012;120(23):4461-4469.

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

MI-2-2

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。

MI-2-2 

MI-2-2 是一种有效的 menin-MLL 抑制剂。MI-2-2 以低纳摩尔亲和力 (Kd=22 nM) 与 menin 结合,并非常有效地破坏 menin 和 MLL 之间的二价蛋白质-蛋白质相互作用。MI-2-2 在 MLL 白血病细胞中具有特异且非常显著的活性,包括抑制细胞增殖、下调 Hoxa9 表达和分化。

MI-2-2

MI-2-2 Chemical Structure

CAS No. : 1454920-20-7

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

MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation[1].

体外研究
(In Vitro)

MI-2-2 is capable of inhibiting both the interaction of menin with MBM1 (IC50= 46 nM) and with the bivalent fragment of MLL that comprises both MBM1 and MBM2 (IC50=520 nM). MI-2-2 exhibits very pronounced activities at low micromolar concentrations in BMCs transformed with MLL-AF9 and in MV4;11, a human leukemia cell line harboring the MLL-AF4 translocation[1].

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

分子量

415.50

Formula

C17H20F3N5S2

CAS 号

1454920-20-7

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]. Shi A, et al. Structural insights into inhibition of the bivalent menin-MLL interaction by small molecules in leukemia. Blood. 2012;120(23):4461-4469.

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

MI-2-2

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。

MI-2-2 

MI-2-2 是一种有效的 menin-MLL 抑制剂。MI-2-2 以低纳摩尔亲和力 (Kd=22 nM) 与 menin 结合,并非常有效地破坏 menin 和 MLL 之间的二价蛋白质-蛋白质相互作用。MI-2-2 在 MLL 白血病细胞中具有特异且非常显著的活性,包括抑制细胞增殖、下调 Hoxa9 表达和分化。

MI-2-2

MI-2-2 Chemical Structure

CAS No. : 1454920-20-7

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

MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation[1].

体外研究
(In Vitro)

MI-2-2 is capable of inhibiting both the interaction of menin with MBM1 (IC50= 46 nM) and with the bivalent fragment of MLL that comprises both MBM1 and MBM2 (IC50=520 nM). MI-2-2 exhibits very pronounced activities at low micromolar concentrations in BMCs transformed with MLL-AF9 and in MV4;11, a human leukemia cell line harboring the MLL-AF4 translocation[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

415.50

Formula

C17H20F3N5S2

CAS 号

1454920-20-7

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]. Shi A, et al. Structural insights into inhibition of the bivalent menin-MLL interaction by small molecules in leukemia. Blood. 2012;120(23):4461-4469.

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

MI-389

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。

MI-389 

MI-389 是一种 PROTAC 翻译终止因子 GSPT1 降解剂。MI-389 破坏了在不同 AML 和 ALL 细胞系中具有共同依赖性的靶点,并且 MI-389 的作用依赖于 CRL4CRBN E3 连接酶。

MI-389

MI-389 Chemical Structure

CAS No. : 2222635-92-7

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

MI-389 is a PROTAC translation termination factor GSPT1 degrader. MI-389 disrupts a target that is a shared dependency in different AML and ALL cell lines, and that MI-389 action is dependent on the CRL4CRBN E3 ligase[1].

IC50 & Target[1]

Cereblon

 

分子量

654.69

Formula

C35H35FN6O6

CAS 号

2222635-92-7

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]. Ishoey M, et al. Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders. ACS Chem Biol. 2018;13(3):553-560.

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

MI-389

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。

MI-389 

MI-389 是一种 PROTAC 翻译终止因子 GSPT1 降解剂。MI-389 破坏了在不同 AML 和 ALL 细胞系中具有共同依赖性的靶点,并且 MI-389 的作用依赖于 CRL4CRBN E3 连接酶。

MI-389

MI-389 Chemical Structure

CAS No. : 2222635-92-7

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

MI-389 is a PROTAC translation termination factor GSPT1 degrader. MI-389 disrupts a target that is a shared dependency in different AML and ALL cell lines, and that MI-389 action is dependent on the CRL4CRBN E3 ligase[1].

IC50 & Target[1]

Cereblon

 

分子量

654.69

Formula

C35H35FN6O6

CAS 号

2222635-92-7

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]. Ishoey M, et al. Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders. ACS Chem Biol. 2018;13(3):553-560.

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

MI-389

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。

MI-389 

MI-389 是一种 PROTAC 翻译终止因子 GSPT1 降解剂。MI-389 破坏了在不同 AML 和 ALL 细胞系中具有共同依赖性的靶点,并且 MI-389 的作用依赖于 CRL4CRBN E3 连接酶。

MI-389

MI-389 Chemical Structure

CAS No. : 2222635-92-7

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

MI-389 is a PROTAC translation termination factor GSPT1 degrader. MI-389 disrupts a target that is a shared dependency in different AML and ALL cell lines, and that MI-389 action is dependent on the CRL4CRBN E3 ligase[1].

IC50 & Target[1]

Cereblon

 

分子量

654.69

Formula

C35H35FN6O6

CAS 号

2222635-92-7

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]. Ishoey M, et al. Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders. ACS Chem Biol. 2018;13(3):553-560.

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

MI-1

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。

MI-1 

MI-1 抑制 Menin-MLL 相互作用,IC50 为 1.9 μM。

MI-1

MI-1 Chemical Structure

CAS No. : 433311-07-0

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

MI-1 inhibits Menin-MLL interaction with an IC50 of 1.9 μM[1].

分子量

387.57

Formula

C19H25N5S2

CAS 号

433311-07-0

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]. Vedadi M, et al. Targeting human SET1/MLL family of proteins. Protein Sci. 2017 Apr;26(4):662-676. doi: 10.1002/pro.3129. Epub 2017 Mar 6.

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

MI-1

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。

MI-1 

MI-1 抑制 Menin-MLL 相互作用,IC50 为 1.9 μM。

MI-1

MI-1 Chemical Structure

CAS No. : 433311-07-0

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

MI-1 inhibits Menin-MLL interaction with an IC50 of 1.9 μM[1].

分子量

387.57

Formula

C19H25N5S2

CAS 号

433311-07-0

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]. Vedadi M, et al. Targeting human SET1/MLL family of proteins. Protein Sci. 2017 Apr;26(4):662-676. doi: 10.1002/pro.3129. Epub 2017 Mar 6.

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

MI-1

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。

MI-1 

MI-1 抑制 Menin-MLL 相互作用,IC50 为 1.9 μM。

MI-1

MI-1 Chemical Structure

CAS No. : 433311-07-0

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

MI-1 inhibits Menin-MLL interaction with an IC50 of 1.9 μM[1].

分子量

387.57

Formula

C19H25N5S2

CAS 号

433311-07-0

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]. Vedadi M, et al. Targeting human SET1/MLL family of proteins. Protein Sci. 2017 Apr;26(4):662-676. doi: 10.1002/pro.3129. Epub 2017 Mar 6.

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

MI-1061

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。

MI-1061  纯度: 99.62%

MI-1061 是一种有效的,口服可生物利用的,化学稳定性的 MDM2 (MDM2-p53 互作) 抑制剂 (IC50=4.4 nM; Ki=0.16 nM)。MI-1061 激活小鼠 SJSA-1 异种移植瘤组织中 p53 并诱导凋亡,具有抗肿瘤活性。

MI-1061

MI-1061 Chemical Structure

CAS No. : 1410737-34-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥12558 In-stock
1 mg ¥5500 In-stock
5 mg ¥9800 In-stock
10 mg ¥15000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

MI-1061 相关产品

相关化合物库:

  • Bioactive Compound Library Plus

生物活性

MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity[1].

IC50 & Target

IC50: 4.4 nM (MDM2)[1]
Ki: 0.16 nM (MDM2)

体外研究
(In Vitro)

MI-1061 achieves IC50=100 and 250 nM in the SJSA-1 and HCT-116 p53+/+ cell lines, respectively, and has IC50>10000 nM in the p53 knockout cell line HCT-116 p53–/–cell line[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)

MI-1061 (100 mg/kg; p.o.; daily for 14 days) is capable of achieving tumor regression in the SJSA-1 xenograft tumor model 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: SCID mice bearing SJSA-1 osteosarcoma xenografts[1]
Dosage: 100 mg/kg
Administration: P.o.; daily for 14 days
Result: Demonstrated strong antitumor activity and achieved significant tumor regression.

分子量

582.45

Formula

C30H26Cl2FN3O4

CAS 号

1410737-34-6

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 : 160 mg/mL (274.70 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7169 mL 8.5844 mL 17.1689 mL
5 mM 0.3434 mL 1.7169 mL 3.4338 mL
10 mM 0.1717 mL 0.8584 mL 1.7169 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: ≥ 4 mg/mL (6.87 mM); Clear solution

    此方案可获得 ≥ 4 mg/mL (6.87 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 40.0 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: 4 mg/mL (6.87 mM); Suspended solution; Need ultrasonic

    此方案可获得 4 mg/mL (6.87 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 40.0 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: ≥ 4 mg/mL (6.87 mM); Clear solution

    此方案可获得 ≥ 4 mg/mL (6.87 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 40.0 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]. Aguilar A, et al. Design of chemically stable, potent, and efficacious MDM2 inhibitors that exploit the retro-mannichring-opening-cyclization reaction mechanism in spiro-oxindoles. J Med Chem. 2014 Dec 26;57(24):10486-98.

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MI-3(Synonyms: Menin-MLL inhibitor 3)

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。

MI-3 (Synonyms: Menin-MLL inhibitor 3) 纯度: 99.73%

MI-3 (Menin-MLL inhibitor 3) 是一种有效且高亲和力的 menin-MLL 抑制剂,IC50 值为 648 nM,Kd 值为 201 nM。

MI-3(Synonyms: Menin-MLL inhibitor 3)

MI-3 Chemical Structure

CAS No. : 1271738-59-0

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 ¥1540 In-stock
5 mg ¥1400 In-stock
10 mg ¥2200 In-stock
50 mg ¥6600 In-stock
100 mg ¥8000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MI-3 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
  • Targeted Diversity Library

生物活性

MI-3 (Menin-MLL inhibitor 3) is a potent and high affinity menin-MLL inhibitor with an IC50 of 648 nM and a Kd of 201 nM[1].

IC50 & Target

IC50: 648 nM (menin-MLL); Kd: 201 nM (menin-MLL)[1]

体外研究
(In Vitro)

MI-3 (12.5-50 μM; HEK293 cells) treatment effectively inhibits the menin-MLL-AF9 interaction in human cells[1].
MI-3 (0-1.6 μM; 72 hours; KOPN-8 and MV4;11 cells) treatment shows an effective and dose-dependent growth inhibition in KOPN-8, MV4 and ME-1 cells[1].
MI-3 (12.5-50 μM; 48 hours; MV4;11 cells) treatment results in a substantial, and dose-dependent increase in Annexin V and AnnexinV/propidium iodide (PI) cells, demonstrating an increase in the number of cells undergoing apoptosis[1].
MI-3 (6.25-25 μM; 6 days; THP-1 cells) treatment results in substantially reduced expression of HOXA9 and MEIS1[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.

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 12.5 μM, 25 μM, 50 μM
Incubation Time:
Result: Very effectively inhibited the menin-MLL-AF9 interaction in human cells.

Cell Viability Assay[1]

Cell Line: KOPN-8 and MV4;11 cells
Concentration: 0 μM, 0.4 μM, 0.8 μM, 1.2 μM, 1.6 μM
Incubation Time: 72 hours
Result: Showed an effective and dose-dependent growth inhibition in KOPN-8 and MV4;11 cells.

Apoptosis Analysis[1]

Cell Line: MV4;11 cells
Concentration: 12.5 μM, 25 μM, 50 μM
Incubation Time: 48 hours
Result: Resulted in an increase in the number of cells undergoing apoptosis.

RT-PCR[1]

Cell Line: THP-1 cells
Concentration: 6.25 μM, 12.5 μM, 25 μM
Incubation Time: 6 days
Result: Resulted in substantially reduced expression of HOXA9 and MEIS1.

分子量

375.55

Formula

C18H25N5S2

CAS 号

1271738-59-0

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 : 8.33 mg/mL (22.18 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6628 mL 13.3138 mL 26.6276 mL
5 mM 0.5326 mL 2.6628 mL 5.3255 mL
10 mM 0.2663 mL 1.3314 mL 2.6628 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: ≥ 0.83 mg/mL (2.21 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (2.21 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 8.3 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.83 mg/mL (2.21 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (2.21 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 8.3 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: ≥ 0.83 mg/mL (2.21 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (2.21 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 8.3 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Grembecka J, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nature Chemical Biology (2012), 8(3), 277-284.

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

MI-463

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。

MI-463  纯度: 99.82%

MI-463是高效,有口服活性的menin-mLL相互作用的小分子抑制剂。

MI-463

MI-463 Chemical Structure

CAS No. : 1628317-18-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1812 In-stock
1 mg ¥700 In-stock
5 mg ¥1700 In-stock
10 mg ¥2700 In-stock
50 mg ¥9900 In-stock
100 mg ¥15800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MI-463 相关产品

相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Reprogramming Compound Library
  • Orally Active Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

体外研究
(In Vitro)

MI-463 can reach the target protein in mammalian cells and effectively inhibit the menin-mLL-AF9 interaction at sub-micromolar concentrations. Treatment of murine bone marrow cells (BMC) transformed with the mLL-AF9 oncogene with MI-463 results in substantial growth inhibition, with GI50 of 0.23 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)

MI-463 achieves high level in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability (45%). Pharmacologic inhibition of the menin-mLL interaction substantially delays progression of mLL leukemia in murine models through on-target activity without causing toxicity. MI-463 induces strong inhibition of tumor growth with once daily intraperitoneal (i.p.) administration. The expression of mLL fusion protein target genes, HOXA9 and MEIS1, are significant reduced upon treatment with MI-463. 20 days treatment of MV4;11 xenograft recipient mice with MI-463 also results in a substantial delay in leukemia progression as manifested by a marked decrease in the bioluminescence level which is associated with a significant decrease in the population of leukemic cells in the peripheral blood, spleen and bone marrow samples[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

484.54

Formula

C24H23F3N6S

CAS 号

1628317-18-9

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 : 125 mg/mL (257.98 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0638 mL 10.3191 mL 20.6381 mL
5 mM 0.4128 mL 2.0638 mL 4.1276 mL
10 mM 0.2064 mL 1.0319 mL 2.0638 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 (4.29 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.29 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 (4.29 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.29 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
  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.29 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.29 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]. Borkin D, et al. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo. Cancer Cell. 2015 Apr 13;27(4):589-602.

Cell Assay
[1]

Leukemia cells are treated with MI-463 or 0.25% DMSO and cultured at 37 °C for 7 days. Media is changed at day 4, viable cell numbers are restored to the original concentration and MI-463 are re-supplied. MTT cell proliferation assay kit is then employed, and plates are read for absorbance at 570 nm using a microplate reader[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: For efficacy studies in MV4;11 subcutaneous xenograft mice model, 5×106 cells are injected into the 4-6 week old female BALB/c nude mice. Treatment is started when the tumor size reached ~100 mm3. Vehicle (25% DMSO, 25% PEG400, 50% PBS) or compounds (MI-463 or MI-503) are administrated once daily at designated doses using i.p. injections[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]. Borkin D, et al. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo. Cancer Cell. 2015 Apr 13;27(4):589-602.

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

MI-538

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。

MI-538  纯度: 99.01%

MI-538是menin和MLL融合蛋白相互作用的抑制剂;IC50值为21 nM。

MI-538

MI-538 Chemical Structure

CAS No. : 1857417-10-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2992 In-stock
5 mg ¥2400 In-stock
10 mg ¥4200 In-stock
25 mg ¥8400 In-stock
50 mg ¥11500 In-stock
100 mg 询价

* Please select Quantity before adding items.

MI-538 相关产品

相关化合物库:

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

生物活性

MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM.

IC50 & Target

IC50 : 21 nM (menin and MLL interaction); Kd: 6.5 nM (menin)[1]

体外研究
(In Vitro)

MI-538 inhibits the proliferation of MLL leukemia cells with a GI50 of 83 nM. MI-538 shows no effect (up to 6 μM) on growth of the control cell lines HL-60 and HM-2, which do not harbor MLL translocations, demonstrating good selectivity toward MLL fusion protein transformed cells. MI-538 binds to menin with low nanomolar affinity (Kd=6.5 nM). Its potent cellular activity originates from the improved binding affinity to menin and possibly increased cell membrane permeability. Treatment with MI-538 results in strong down regulation of expression of Hoxa9 and Meis1 genes. About 100 nM 27 was sufficient to reduce by ~50% Hoxa9 expression in MLL-AF9 cells, and even more pronounced effect was seen on Meis1 expression[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)

Treatment with MI-538 results in a pronounced, about 80%, reduction in the MV4;11 tumor volume, without causing substantial signs of toxicity reflected by less than 10% reduction of the body weight. MI-538 demonstrates markedly improved exposure (area under the curve, AUC, values), Cmax (maximum compound concentration) in the blood plasma, and the lowest value of clearance. The half-life of MI-538 is about 1.6 h. MI-538 has also high oral bioavailability (~50%)[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

566.60

Formula

C27H25F3N8OS

CAS 号

1857417-10-7

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 : 100 mg/mL (176.49 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7649 mL 8.8246 mL 17.6491 mL
5 mM 0.3530 mL 1.7649 mL 3.5298 mL
10 mM 0.1765 mL 0.8825 mL 1.7649 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: ≥ 10 mg/mL (17.65 mM); Clear solution

    此方案可获得 ≥ 10 mg/mL (17.65 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 100.0 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: ≥ 10 mg/mL (17.65 mM); Clear solution

    此方案可获得 ≥ 10 mg/mL (17.65 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 100.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 3.

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

    Solubility: 2.08 mg/mL (3.67 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (3.67 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]. Borkin D, et al. Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL). J Med Chem. 2016 Feb 11;59(3):892-913.

Cell Assay
[1]

MOLM-13, MV4;11, HL-60 human leukemia cells as well as MLL-AF9 and HM-2 murine bone marrow cells are treated with MI-538 or 0.25% DMSO for 7 days. Media are changed at day 4 with viable cell number restored to the original concentration, and MI-538 are resupplied. An amount of 100 μL of cell suspension is transferred to 96-well plates for each sample in quadruplicates. Cell viability is measured using the MTT assay. Plates are read for absorbance at 570 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.

Animal Administration
[1]

Mice: Mice xenograft are randomly grouped with each group containing eight mice. Vehicle or MI-538 (45 mg/kg) are administrated once daily at designated doses using ip injections for 2 weeks. Body weight and tumor sizes are monitored three times a week[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]. Borkin D, et al. Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL). J Med Chem. 2016 Feb 11;59(3):892-913.

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

MI-3454

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。

MI-3454  纯度: 99.79%

MI-3454 是一种具有口服活性,高效和选择性的 Menin-MLL1 相互作用抑制剂,IC50 为 0.51 nM。MI-3454 通过下调涉及白血病发生的关键基因,在 MLL1 重排或 NPM1 突变的白血病小鼠模型中抑制细胞增殖,诱导分化并完全缓解或消退白血病。

MI-3454

MI-3454 Chemical Structure

CAS No. : 2134169-43-8

规格 价格 是否有货 数量
5 mg ¥6200 In-stock
10 mg ¥9800 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

MI-3454 相关产品

相关化合物库:

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

生物活性

MI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis[1].

IC50 & Target

IC50: 0.51 nM (menin-MLL1 interaction)[1]

体外研究
(In Vitro)

MI-3454 (0.001-10 μM; 7 days) strongly reduces murine bone marrow cells transformed with MLL-AF9 or Hoxa9/Meis1 proliferation[1].
MI-3454 (50 nM; 6 days) leads to downregulated expression of HOXA9 and MEIS1 in Human leukemic cell lines MV-4-11 cells or MOLM13[1].
MI-3454 markedly reduces the viability of leukemic cells harboring various MLL fusion proteins (MLL-AF9, MLL-AF4, MLL-ENL), with GI50 values ranging from 7 to 27 nM. MI-3454 blocks the interaction of menin with an MLL14–43 fragment encompassing the entire menin binding motif[1].
MI-3454 does not potently inhibit cytochromes P450 (<50% inhibition at 10 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 Proliferation Assay[1]

Cell Line: Murine bone marrow cells transformed with MLL-AF9 or Hoxa9/Meis1
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 7 days
Result: Demonstrated strong reduction of cell proliferation.

RT-PCR[1]

Cell Line: Human leukemic cell lines MV-4-11 cells or MOLM13
Concentration: 50 nM
Incubation Time: 6 days
Result: Led to downregulated expression of HOXA9 and MEIS1 and expression level of other MLL fusion target genes, including MEF2C, DLX2, HOXA10, PBX3, and FLT3.

体内研究
(In Vivo)

MI-3454 induces complete remission or regression of leukemia in mouse models of mixed lineage leukemia 1 (MLL1)-rearranged or nucleophosmin 1 (NPM1)-mutated leukemia[1].
MI-3454 (p.o.; 120 mg/kg; one or twice daily for 7 consecutive days) sufficiently blocks leukemia progression by a once-daily treatment[1].
MI-3454 (p.o.; 100 mg/kg; b.i.d.; for 19 consecutive days) effectively blocks leukemia progression during the treatment period and markedly prolongs survival of MOLM13 xenotransplantation model mice. MI-3454 induces complete remission or blocks leukemia progression in patient-derived xenograft (PDX) models of MLL leukemia[1].
MI-3454 (100 mg/kg of PO or 15 mg/kg of IV) has a T1/2 of 3.2 hours, a Cmax of 4698 mg/mL for PO[1].
MI-3454 exhibits favorable stability in murine and human liver microsomes (t1/2=20.4 minutes and 37.1 minutes, respectively)[1].
MI-3454 demonstrates lower levels in brain and cerebrospinal fluid, suggesting limited ability to cross the blood-brain barrier[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: 8- to 10-week-old female NSG mice (MV-4-11 xenotransplantation model of MLL leukemia)[1]
Dosage: 120 mg/kg
Administration: Orally; one or twice daily for 7 consecutive days
Result: A once-daily treatment was sufficient to block leukemia progression.
Animal Model: Female CD-1 mice[1]
Dosage: 100 mg/kg (PO) or 15 mg/kg (IV) (Pharmacokinetic Analysis)
Administration: PO or IV
Result: Had a T1/2 of 3.2 hours, a Cmax of 4698 mg/mL for PO.
Had a T1/2 of 2.4 hours, a CL of 2375 mL/hours•kg, and a Vss of 5358 mL/kg for IV.

分子量

636.73

Formula

C32H35F3N8OS

CAS 号

2134169-43-8

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 : 31.25 mg/mL (49.08 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5705 mL 7.8526 mL 15.7052 mL
5 mM 0.3141 mL 1.5705 mL 3.1410 mL
10 mM 0.1571 mL 0.7853 mL 1.5705 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。

参考文献
  • [1]. Szymon Klossowski, et al. Menin Inhibitor MI-3454 Induces Remission in MLL1-rearranged and NPM1-mutated Models of Leukemia. J Clin Invest. 2020 Feb 3;130(2):981-997.

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

MI培养基

上海金畔生物科技有限公司可以定制生产国产培养基,可以访问官网了解更多产品信息。
MI培养基

英文名称: MI Medium
产品货号: JP8686
产品规格: 1000ml
900元
保质期: 三年
产品用途: 用于滤膜法计数饮用水中大肠埃希氏菌和大肠菌群
备  注:

产品介绍:

用途:用于滤膜计数饮用水中大肠埃希氏菌和大肠菌群。

用法

称取本品 36.5g,加热溶解于 1000ml 蒸馏水中,分装三角瓶,每瓶 200ml,121℃高压灭菌 15min,冷至 50℃左右时,每瓶加入一支头孢磺啶钠(1mg/支),混匀,倾入无菌平皿,备用。

实验原理:

MI琼脂中的蛋白胨可以为细菌生长提供氮、碳和氨基酸。酵母提取物提供微量元素,维生素和氨基酸。乳糖是一种可发酵的碳水化合物碳源。氯化钠保持渗透平衡。磷酸一钾和磷酸二钾具有缓冲作用。十二烷基硫酸钠和去氧胆酸钠可抑制革兰氏阳性细菌。

大肠杆菌产生的β-D-葡萄糖醛酸酶将显色剂吲哚氧基-β-D-葡萄糖醛酸(IBDG)切割成蓝色或靛蓝色化合物。大肠菌群产生的β-半乳糖苷酶可裂解氟化物4-甲基伞形酮-β-D-葡萄糖醛酸苷,生产4-甲基伞形酮,一种荧光化合物,当暴露于长波紫外线(366nm)时,可出现荧光反应。琼脂作为固化剂。

头孢磺啶钠可抑制革兰氏阳性细菌和一些非大肠菌群革兰氏阴性细菌生长。

MI培养基质控结果:

MI培养基的微生物灵敏度试验:

按标签用法制备培养基,接种以下质控菌株,放置35±2℃需氧培养20-24小时。
注:回收率计算时,用TSA琼脂做对照培养基。

MI培养基原理及实验现象 .aspasphtml/refere10582.htm


MI培养基相关产品:

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E.Coli Broth
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Lactose Bile Broth
250g 用于大肠菌群,粪大肠菌群,大肠杆菌的测定(GB标准)
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Lactose Broth
250g 用于大肠菌群,粪大肠菌群,大肠杆菌的测定(GB标准)
JP0112 去氧胆酸盐琼脂(DC)
Desoxycholate Lactose Agar
250g 用于大肠菌群固体平板测定
JP0113 MR-VP培养基
Methyl Red Voges Proskauer Broth
250g 用于大肠杆菌的甲基红实验和VP实验
JP0114 结晶紫中性红胆盐琼脂(VRBA)
Violet Red Bile Agar
250g 用于大肠菌群的固体平板检测(GB、SN标准)
JP0116 肠道菌计数琼脂(VRBDA)
Violet Red Bile Dextrose Agar
250g 用于肠道菌计数和肠杆菌科鉴别
JP0118 品红亚硫酸钠琼脂
Fuchsin Basic Sodium Sulfite Agar
250g 用于饮用水,水源水中总大肠菌群的选择性分离和确证(GB标准)
JP0119 乳糖蛋白胨培养液
Lactose Peptone Broth
250g 用于饮用水,水源水中总大肠菌群的测定
JP0126 肠道菌增菌肉汤(EE)
Enterobacteria Enrichment Broth
250g 用于肠道菌的增菌培养(GB标准)
JP0128 LB肉汤
LB Broth
250g 用于分子生物学中大肠杆菌的培养
JP0129 LB营养琼脂
LB Nutrient Agar
250g 用于分子生物学中大肠杆菌的培养
GB095 苯丙氨酸脱氨酶
Phenylalanine Deaminase Medium
20支/盒 用于苯丙氨酸脱氨酶试验(需添加苯丙氨酸指示剂配套使用)
JP0107 伊红美蓝琼脂(EMB)
Eosin-Methylene Blue Agar
250g 弱选择性培养基、用于分离肠道致病菌,特别是大肠杆菌(GB、SN标准)
JP8279 Kovacs氏靛基质试剂盒
Kovacs’s indole kit
5ml*2 用于吲哚(靛基质)试验
JP8280 甲基红试剂盒
Methyl Red Indicator Box
5ml*2 用于甲基红试验
JP0131 哥伦比亚MUG培养基
Columbia- MUG Medium
250g 用于大肠杆菌的荧光检测(SN标准)
JP0134 BDS培养基
BDS Medium
250g 用于培养拟杆菌
JP0135 葡萄糖琼脂
Dextrose Agar
250g 用于细菌的综合生化试验(不含溴甲酚紫)
JP0136 Andrade氏糖类肉汤
Andrade’s Carbohydrate Broth
250g 用于细菌的糖发酵试验
JP0137 Korser氏枸椽酸盐肉汤
Korser Citrate Sodium Broth
100g 用于细菌枸椽酸盐试验(SN标准)
JP0138 Endo培养基
Endo Agar
250g 用于滤膜法测定生活饮用水及其水源水中的总大肠菌群
JP0140 乳糖莫能霉素葡萄糖醛酸琼脂
LMG Agar
250g 用于滤膜MUG法检测食品中大肠菌群数(SN/T1059.2)
JP0143 Tergitol-7琼脂
Tergitol-7 Agar
250g 用于大肠菌群的鉴定
JP0152 A-1培养基
A1 Medium
250g 用于水中粪大肠菌群检测
JP0161 Les Endo琼脂
m-Endo Agar,LES
250g 用于水中大肠菌群滤膜法计数
JP0163 m-TEC琼脂
m-TEC Agar
250g 用于水中耐热细菌滤膜计数
JP0164 现隐肉汤
Presence Absence Broth
250g 用于水中大肠菌群计数(US-EPA方法)
JP0168 心浸液琼脂
Heart Infusion Agar
250g 用于培养营养要求高的微生物
JP0169 桔汁琼脂(也叫橙血清琼脂 OSA)
Orange Serum Agar
250g 用于饮料中耐酸细菌的分离培养
JP0171 EEM培养基
EEM medium
250g 用于致病性大肠杆菌的增菌培养和肠杆菌的增菌培养
JP0172 胰蛋白胨胆盐琼脂
Tryptone Bile Agar
250g 用于大肠杆菌的膜过滤法选择性培养(ISO标准)
JP8516 Elek氏培养基
Elek Medium
250g 用于致泻大肠埃希氏菌的产毒培养
JP0143 Tergitol-7琼脂
Tergitol-7 Agar
250g 用于大肠菌群的鉴定(NMKL)
JP0154-1 MFC肉汤
MFC Broth
250g 用于生活饮用水及其水源水中粪大肠菌群测定
JP0154 MFC琼脂
MFC Agar
250g 用于粪大肠菌群的滤膜法检测
JP0104 煌绿乳糖胆盐肉汤(BGLB)
Brilliant Green Lactose Bile Broth
250g 用于大肠菌群、大肠杆菌的测定(GB、SN标准)
JP8281 V-P试剂盒
V-P Box
5ml*4 用于V-P试验
JP8507-1 PBS缓冲液(pH7.3)
PBS
250g 用于样品制备的稀释剂
JPY8308 MEE肉汤
MEE Broth
250g 用于肠道菌的选择性增菌培养(SN标准)
JP8675 TTC乳糖琼脂
Lactose TTC agar
250g 滤膜法检测水中大肠杆菌和大肠菌群
JP0116-2 结晶紫中性红胆盐肉汤
Neutral Red-bile Salt Peptone Glucose Medium
250g 用于肠道菌增菌培养
JP0112-1 大肠菌群培养基(日本)
Coliform Medium(Japan)
250g 用于大肠菌群的固体平板检测
JP8536-1 艾格LT100肉汤 250g 用于化妆品中好氧菌的增菌培养
JP0108-2 营养肉汤(日本标准)
Nutrient Broth(Japan)
250g 用于一般细菌培养、转种、复壮、增菌等
JPDC002 SOC培养基
SOC Medium
250g 用于基因工程菌大肠杆菌培养
JP0141-1 茜素-β-半乳糖苷肉汤(Aliz-gal肉汤)
Aliz-gal Broth
100g 用于食品中大肠菌群快速检测
JP0109-6 营养琼脂(琼脂20g)
Nutrient Agar(Agar 20g)
250g 用于样品中菌落总数的计数
JP0113 MR-VP培养基
Methyl Red Voges Proskauer Broth
250g 用于大肠杆菌的甲基红实验和VP实验
JP0158 去氧胆酸盐枸橼酸盐乳糖蔗糖琼脂
DCLS Agar
250g 用于沙门氏菌和志贺氏菌的分离培养
JP8517 Honda氏产毒肉汤
Honda Toxin-Producing Broth
250g 用于致泻大肠埃希氏菌的产毒培养
JP8278 革兰氏染色液试剂盒
Gram Stain Kit
5ml*8 用于细菌的革兰氏染色试验
JP7001 大肠杆菌显色培养基
E. coli Chromogenic Medium
1000ml 用于大肠杆菌的显色快速培养
JP7002 大肠菌群显色培养基
Coliform Chromogenic Medium
1000ml 用于快速、准确检测大肠菌群,培养24小时,大肠菌群显蓝绿色
JP8562 MSA培养基
MSA Medium
250g 用于肠球菌,轻型链球菌和唾液链球菌分离培养
JP0108-3 营养肉汤(GB/T20944.1-2007纺织品标准)
Nutrient Agar
250g 一般细菌培养,转种,复壮,增菌等,也可用于消毒效果检测
JPPT8621-1 磷酸盐缓冲液 (PBS pH7.2) 9ml*20支/盒 用于菌落总数,大肠菌群,金葡菌,大肠杆菌样品制备
JP8720 ModifiedSclohtens’Broth(MSB)
Modified Sclohtens’ Broth
250g 用于阴沟肠杆菌的培养
JP8722 葡萄糖肉汤
Dextrose Broth
250g 用于营养苛求菌培养和肠道菌产气实验
JP8726 最小肉汤培养基
the Smallest Broth Medium
250g
JPPT020 EC肉汤(含小倒管) 9ml*20支/盒 用于粪大肠菌群、大肠杆菌的测定
JP8720 ModifiedSclohtens’Broth(MSB)
Modified Sclohtens’ Broth
250g 用于阴沟肠杆菌的培养
JP0169 桔汁琼脂(也叫橙血清琼脂 OSA)
Orange Serum Agar
250g 用于饮料中耐酸细菌的分离培养
JPDC006 JP-PET自诱导培养基
JP-PET Auto-Indection Medium
250g 用于基因工程菌大肠杆菌自诱导蛋白表达培养
JP0138-2 m-远藤氏培养基
M-Endo Medium
250g 用于滤膜法检测水中大肠菌群
JP8774 CAYE培养基
CAYE Medium
250g 用于致病性大肠埃希氏菌的产毒培养
JP8773 接种测试微生物琼脂培养基
Medium Ⅱ(for Transferring the Test Organism)
250g 用于抗生素效价测定
JP8772 菌种和底层琼脂培养基
Medium I(foe Seed and Basal Layer)
250g 用于抗生素效价测定的底层培养基或菌种活化
JP0102-3 双料月桂基硫酸盐胰蛋白胨肉汤(LST)
Double Lauryl Sulfate Tryptose Broth
250g 用于大肠菌群,大肠杆菌的测定(GB、SN标准)
JP8797 消毒液中和肉汤
Disinfectant Neutralization Broth
250g 用于中和醇类、酚类消毒剂、含氯消毒剂、含碘消毒剂、过氧化物消毒剂、季铵盐类消毒剂、醛类消毒剂等
JP8798 卵磷脂吐温稀释液
Lecithin polysorbate(LP)diluent
250g 用于样品制备水稀释
JP0152 A-1培养基
A-1 Medium
250g 用于水中粪大肠菌群检测
JP8807 M-Endo肉汤
M-Endo Broth
250g 用于滤膜法计数水中大肠菌群
JP8808 CCFA琼脂基础
CCFA Agar Base
250g 用于艰难梭菌选择性分离培养
JP8774 CAYE培养基
CAYE Medium
250g 用于致病性大肠埃希氏菌的产毒培养
JP0114-5k 结晶紫中性红胆盐琼脂(VRBA)
Violet Red Bile Agar
5kg 用于大肠菌群的固体平板检测(GB、SN标准)
JP0135-2 葡萄糖琼脂
Dextrose Agar
250g 用于肠杆菌科细菌葡萄糖发酵试管(国内常用)
JP0136 Andrade氏糖类肉汤
Andrade’s Carbohydrade Broth
250g 用于细菌的糖发酵试验
JP0154-1 MFC肉汤
MFC肉汤
250g 用于生活饮用水及其水源水中粪大肠菌群测定
JP5188-2 双料乳糖胆盐发酵培养基
Double Lactose Bile Medium
250g 用于大肠杆菌、粪大肠菌群、大肠杆菌的测定
JP8414-2 肠道菌增菌肉汤(USP)
Mossel-Enterobacteriaceae Enrichment Broth
250g 用于肠杆菌科细菌的选择性增菌培养
JP0116-1 紫红胆盐葡萄糖琼脂(EP7.0)
Violet Red Bile Glucose Agar
250g 用于肠道菌计数和肠杆菌科鉴别
JP0126-5 肠道菌富集肉汤培养基(USP)
Enterobacteria enrichment broth-Mossel Medium
250g 用于肠杆菌科细菌的选择性增菌培养
JP8643-1 革兰氏阴性菌增菌液
Gram Negative Bacteria Enrichment Broth
250g 用于革兰氏阴性细菌增菌培养
JP8780 大肠杆菌噬菌体MS2液体培养基
Coliphage MS2 Liquid Medium
250g 用于大肠杆菌噬菌体MS2培养
JP8782 大肠杆菌噬菌体MS2半固体培养基
Coliphage MS2 Medium(Semisolid)
250g 用于大肠杆菌噬菌体MS2培养
JP8806 GAD培养基
GAD Medium
250g
JPD0259 阴沟肠杆菌分离琼脂(ECIA)
Enterobacter Cloacae Isolation Agar
100g 用于乳及乳制品中阴沟肠杆菌分离培养
JP0177-2 胰蛋白胨大豆琼脂(TSA)(ISO9038-1-2000)
Tryptone Soy Agar
250g 用于大肠杆菌培养
JP0172-1 胰蛋白胨胆盐琼脂(TBA)(ISO9038-1-2000)
Tryptone Bile Agar
250g 用于大肠杆菌确证试验
JP8858 胰化大豆硫酸镁琼脂(TSAM)
Tryptic Soy Aagr w/Magnesium Sulfate
250g 用于HGMF膜法培养大肠菌群
JPKP6238-10 麦康凯琼脂培养基(颗粒)(中国药典)
MacConkey Agar
250g 用于大肠埃希菌的选择性分离培养
JPPM8686 MI琼脂培养基平板
MI Medium Plate
9cm*10个 用于滤膜法计数饮用水中大肠埃希氏菌和大肠菌群
JP8520-1 大豆酪蛋白消化物卵磷脂吐温80琼脂培养基(SCDCPA)
SCDCPA
250g 用于环境、器皿、设备和表面的无菌检测
JP8528 营养肉汁琼脂
Nutrient Agar
250g 用于一般细菌复苏和纯化培养
JPPT0135-2 葡萄糖琼脂斜面管 20支/盒 用于肠杆菌科细菌葡萄糖发酵试验
JP0126-7 缓冲葡萄糖煌绿胆盐肉汤(EE肉汤)
EE Broth
250g 用于肠杆菌科的选择性增菌培养
JP0176-4 结晶紫中性红胆盐葡萄糖琼脂(VRBGA)(GB4789.41-2016)
Violet Red Bile Glucose Agar
250g 用于肠杆菌科的分离培养
GB144-1 果糖 20支/盒 用于细菌的果糖发酵实验
JP6238-4 麦康凯琼脂(不含氯化钠和结晶紫)
MacConkey Agar
250g 用于革兰氏阴性菌的分离培养(抑制变形杆菌的漫延)
JPPM6238-11 麦康凯琼脂培养基平板(9cm)
MacConkey Agar Medium Plate
9cm*10个/包 用于大肠埃希氏菌的分离培养
JPPM6238-10 麦康凯琼脂培养基平板(9cm)(中国药典)
MacConkey Agar Plate
9cm*10个/包 用于大肠埃希氏菌的分离培养
JPPP022-50 50ml三倍乳糖胆盐发酵培养基
50ml Triple Lactose Bile Broth
50ml*20瓶 用于大肠杆菌、粪大肠菌群、大肠杆菌的测定
JPPT0126 30ml肠道菌增菌肉汤
30ml Enterobacteria Enrichment Broth
30ml*20 用于肠杆菌科细菌的增菌培养
JP8304 PW稀释液
PW Broth
250g 用于检测肠杆菌时制备样品的稀释液
JP0114-7 结晶紫中性红胆盐-4-甲基伞形酮-β-D-葡萄糖苷琼脂(VRBA-MUG)
VRBA-MUG
100g 用于大肠杆菌酶底物法平板计数
JP0115 西蒙氏枸橼酸盐琼脂
Simmons Citrate Agar
250g 用于肠道菌的柠檬酸盐利用试验(GB标准)
JP8643a 青霉素溶液 1ml*5支 作为JP8643的添加剂使用
JP0110-4 乳糖胆盐培养液
Lactose Bile Broth
250g 用于医疗机构污水和污泥中粪大肠菌群检测
JPBD0114-200 结晶紫中性红胆盐琼脂(VRBA) 袋装即用型
Violet Red Bile Agar
200ml/袋*10 用于大肠菌群的固体平板检测(GB、SN标准)
JPPT0111 乳糖复发酵管
Lactose Broth Tube
10ml*20支 用于大肠菌群,粪大肠菌群,大肠杆菌的测定(GB标准)

MI-503

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。

MI-503  纯度: 99.81%

MI-503是高效,有口服活性的menin-mLL相互作用的小分子抑制剂。

MI-503

MI-503 Chemical Structure

CAS No. : 1857417-13-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1615 In-stock
2 mg ¥650 In-stock
5 mg ¥1300 In-stock
10 mg ¥2300 In-stock
25 mg ¥4900 In-stock
50 mg ¥7900 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

MI-503 相关产品

相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Reprogramming Compound Library
  • Orally Active Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

体外研究
(In Vitro)

MI-503 occupies the F9 and P13 pockets on menin, forming a hydrogen bond with Tyr276, and also extends beyond the P13 pocket to form hydrogen bonds with Trp341 and Glu366. Treatment of murine bone marrow cells (BMC) transformed with the mLL-AF9 oncogene with MI-503 results in substantial growth inhibition, with GI50 of 0.22 μM. The cell growth inhibitory effect of MI-503 is time-dependent, with a pronounced effect achieved after 7-10 days of treatment[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)

MI-503 achieves high level in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability (75%). MI-503 induces strong inhibition of tumor growth with once daily intraperitoneal (i.p.) administration. Treatment with MI-503 results in an over 80% reduction in MV4;11 tumor volume and complete tumor regression in two mice. Ten consecutive days of treatment with MI-503 results in a marked delay in progression of mLL leukemia in mice and significantly reduces leukemia tumor burden. Treatment with MI-503 and MI-463 leads to markedly reduced expression of Hoxa9 and Meis1, downstream targets of mLL fusion proteins substantially upregulated in mLL leukemias[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

564.63

Formula

C28H27F3N8S

CAS 号

1857417-13-0

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 : 25 mg/mL (44.28 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7711 mL 8.8554 mL 17.7107 mL
5 mM 0.3542 mL 1.7711 mL 3.5421 mL
10 mM 0.1771 mL 0.8855 mL 1.7711 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 (3.68 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.68 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 (3.68 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.68 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]. Borkin D, et al. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo. Cancer Cell. 2015 Apr 13;27(4):589-602.

Cell Assay
[1]

Leukemia cells are treated with MI-503 or 0.25% DMSO and cultured at 37 °C for 7 days. Media is changed at day 4, viable cell numbers are restored to the original concentration and MI-503 are re-supplied. MTT cell proliferation assay kit is then employed, and plates are read for absorbance at 570 nm using a microplate reader[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: For efficacy studies in MV4;11 subcutaneous xenograft mice model, 5×106 cells are injected into the 4-6 week old female BALB/c nude mice. Treatment is started when the tumor size reached ~100 mm3. Vehicle (25% DMSO, 25% PEG400, 50% PBS) or compounds (MI-463 or MI-503) are administrated once daily at designated doses using i.p. injections[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]. Borkin D, et al. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo. Cancer Cell. 2015 Apr 13;27(4):589-602.

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