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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Haspin Kinase-CHR6494 trifluoroacetate
CHR6494 trifluoroacetate

Chemical Structure : CHR6494 trifluoroacetate

CAS No.: 1458630-17-5

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CHR6494 trifluoroacetate (CHR6494 TFA)

货号: PC-49322Not For Human Use, Lab Use Only.

CHR-6494 (CHR6494) trifluoroacetate is a potent, selective inhibitor of the histone kinase Haspin with IC50 of 2 nM, shows anti-proliferative effects in human cancer cells.

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

生物&药学活性

CHR-6494 (CHR6494) trifluoroacetate is a potent, selective inhibitor of the histone kinase Haspin with IC50 of 2 nM, shows anti-proliferative effects in human cancer cells.
CHR-6494 displays selectivity over 27 other protein kinases including Aurora B kinase.
CHR-6494 inhibits cancer cell growth dose dependently with IC50 500 nM for HCT-116, 473 nM for HeLa and 752 nM for MDA-MB-231 cells.
CHR-6494 reduces H3T3ph levels in a dose-dependent manner and causes a mitotic catastrophe characterized by metaphase misalignment, spindle abnormalities and centrosome amplification.
CHR-6494 causes arrest in G2/M and subsequently apoptosis in cancer cells.
CHR-6494 demonstrates anti-angiogenetic features in ex vivo assays, shows antitumor potential in xenografted nude mice without any observed toxicity in vivo.

物理化学性质&存储条件

分子量 406.369
分子式 C18H17F3N6O2
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-(1H-indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine trifluoroacetate

参考文献

1. Huertas D, et al. Oncogene. 2012 Mar 15;31(11):1408-18.

2. Han L, et al. J Cancer. 2017 Aug 25;8(15):2933-2943.

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