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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-ERK-CC-90003
CC-90003

Chemical Structure : CC-90003

CAS No.: 1621999-82-3

CC-90003 (CC90003)

货号: PC-35813Not For Human Use, Lab Use Only.

CC-90003 (CC90003) is a potent and selective, covalent ERK1/2 inhibitor with IC50 of 10-20 nM, demonstrates excellent selectivity in a 258-kinase biochemical assay panel.

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10 mg ¥1880 In stock
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50 mg ¥4980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CC-90003 (CC90003) is a potent and selective, covalent ERK1/2 inhibitor with IC50 of 10-20 nM, demonstrates excellent selectivity in a 258-kinase biochemical assay panel.
CC-90003 potently inhibits 27 growth of KRAS mutant cell lines with GI50 of <1 uM, also is active against 28 of 37 (76%) KRAS-mutant cancer cell lines.
CC-90003 shows cytotoxic effects in KRAS mutant PDAC, lung cancer and CRC cell lines, does not significantly inhibit proliferation of normal lung fibroblasts or bronchial epithelial cells.
CC-90003 decreases colony formation ex-vivo and inhibits tumor growth in vivo of KRAS mutant PDX models, induces full regression and prevents regrowth of KRAS mutant Lung PDX model when combined with Docetaxel.

物理化学性质&存储条件

分子量 458.445
分子式 C22H21F3N6O2
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

N-(2-((2-((2-methoxy-5-methylpyridin-4-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)-5-methylphenyl)acrylamide

参考文献

1. Aronchik I, et al. Mol Cancer Res. 2018 Oct 1. pii: molcanres.0554.2017. doi: 10.1158/1541-7786.MCR-17-0554.

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