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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-CCT251545
CCT251545

Chemical Structure : CCT251545

CAS No.: 1661839-45-7

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CCT251545 (CCT 251545;CCT-251545)

货号: PC-43145Not For Human Use, Lab Use Only.

CCT251545 is a potent, orally bioavailable inhibitor of Wnt signaling with IC50 of 5 nM, also is a potent and selective chemical probe for CDK8 and CDK19 with >100-fold selectivity over 291 other kinases.

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

生物&药学活性

CCT251545 is a potent, orally bioavailable inhibitor of Wnt signaling with IC50 of 5 nM, also is a potent and selective chemical probe for CDK8 and CDK19 with >100-fold selectivity over 291 other kinases.
CCT251545 potently inhibits reporter-based readouts of basal WNT pathway activity in LS174T and SW480 cells in the absence of WNT ligand with IC50 of 23 and 190 nM, respectively.
CCT251545 demonstrates potent inhibition of WNT pathway activity in APC mutant human colorectal cancer cell line with IC50 of 35 nM.
CCT251545 inhibits phospho-STAT1SER727 levels in SW620 cells with IC50 of 9 nM.
CCT251545 demonstrate in vivo activity in WNT-dependent tumors.

物理化学性质&存储条件

分子量 421.9225
分子式 C23H24ClN5O
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

DMSO: ≥ 50 mg/mL
Chemical Name/SMILES

2,8-Diazaspiro[4.5]decan-1-one, 8-[3-chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]-4-pyridinyl]-

参考文献

1. Mallinger A, et al. J Med Chem. 2015 Feb 26;58(4):1717-35.

2. Dale T, et al. Nat Chem Biol. 2015 Dec;11(12):973-980.

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