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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-SNX631
SNX631

Chemical Structure : SNX631

CAS No.: 868066-26-6

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SNX631 (SNX-631)

货号: PC-49204Not For Human Use, Lab Use Only.

SNX631 (SNX-631) is a potent, selective inhibitor of CDK8/19 Mediator kinase with IC50 of 10.3 nM in the NF κB-dependent cell-based assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SNX631 (SNX-631) is a potent, selective inhibitor of CDK8/19 Mediator kinase with IC50 of 10.3 nM in the NF κB-dependent cell-based assays.
SNX631 is 6 to 10 times more potent than Senexin B in all the assays except for the DiscoverX activesite-dependent competition binding assay.
SNX631 showed synergistic interactions with lapatinib and trastuzumab in a panel of HER2+ BrCa cell lines, overcoming and preventing resistance to HER2-targeting drugs.
Combination of HER2-mAb trastuzumab and SNX631 inhibited STAT1 and STAT3 phosphorylation at S727 and up-regulated tumor suppressor BTG2 in HER2+ BrCa cell lines.
SNX631 partially inhibits growth of xenograft tumors formed by lapatinib-sensitive or -resistant HER2+ breast cancer cells alone, and strongly suppressed by the combination of lapatinib, overcoming lapatinib resistance.

物理化学性质&存储条件

分子量 438.550
分子式 C22H26N6O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-amino-4-(4-(4-(dimethylcarbamoyl)phenyl)-1,4-diazepan-1-yl)thieno[2,3-b]pyridine-2-carboxamide

参考文献

1. Jing Li, et al. Cells. 2019 Oct 6;8(10):1208.

2. Xiaokai Ding, et al. Proc Natl Acad Sci U S A. 2022 Aug 9;119(32):e2201073119.

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