WDR5 inhibitor 10

Chemical Structure : WDR5 inhibitor 10

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货号: PC-49598Not For Human Use, Lab Use Only.

WDR5 inhibitor 10 is a highly potent, selective and orally active inhibitor of WD repeat domain 5 (WDR5) with TR-FRET Ki value of <0.02 nM, shows potent antiproliferative activity with GI50 of 9.7 nM in MV4:11 cells.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

WDR5 inhibitor 10 is a highly potent, selective and orally active inhibitor of WD repeat domain 5 (WDR5) with TR-FRET Ki value of <0.02 nM, shows potent antiproliferative activity with GI50 of 9.7 nM in MV4:11 cells.
WDR5 inhibitor 10 binds in the WDR5 WIN site.
WDR5 inhibitor 10 (50-150 mg/kg, oral) demonstrated antitumor effects in an MV4:11 subcutaneous tumor xenograft model.
WDR5 inhibitor 10 showed dose-dependent suppression of universal RPG targets of WDR5 (RPL26, RPL32, RPL35, RPS14, and RPS24) transcripts in MV4:11 cells.
WDR5 inhibitor 10 is well-tolerated in rats up to 100 mg/kg BID dose over the 7-d study without serious adverse effects.

物理化学性质&存储条件

分子量	587.61
分子式	C31H28F3N7O2
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	4-(7-((1H-imidazol-1-yl)methyl)-5-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)-1-oxo-3,4-dihydroisoquinolin-2(1H)-yl)-6-ethyl-N-methylquinoline-8-carboxamide

参考文献

1. Teuscher KB, et al. Proc Natl Acad Sci U S A. 2023 Jan 3;120(1):e2211297120.