MK-1775

货号：M3434

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。

 

产品描述

 

Wee1 is a cellular protein kinase which inhibits Cdc2 activity, thereby preventing cells from proceeding through mitosis by maintaining G2 arrest. MK-1775 (AZD1775) is a first-in-class, pyrazolo-pyrimidine derivative and potent small-molecule inhibitor of Wee1 kinase with IC₅₀ of 5.2 nM and blocks G2 DNA damage checkpoint. In vitro, MK-1775 treatment at 500 nM for 48h caused S arrest or both S and G2/M arrest in human pancreatic cancer cell lines AsPC-1, BxPC-3, CFPAC-1, HPAC, MIAPaCa-2 and PANC-1. In vivo, MK-1775 (20 mg/kg) twice daily combined with and panobinostat (10 mg/kg) once daily treatment in mice bearing BxPC-3 xenograft tumors, resulted in significant delay of tumor growth during the treatment period compared to single drug treatment, with 58.7% tumor growth inhibition on day 20. The combination of gemcitabine (100 mg/kg, i.p., twice weekly on days 1 and 4, for 4 weeks) with MK-1775 (30 mg/kg. p.o., once daily for 4 weeks) produced robust antitumor activity and remarkably enhanced tumor regression response (4.01-fold) compared to gemcitabine treatment in p53-deficient tumors.

 

储存液制备	质量	1 mg	5 mg	10 mg
	1 mM	1.9976 mL	9.9881 mL	19.9762 mL
	5 mM	0.3995 mL	1.9976 mL	3.9952 mL
	10 mM	0.1998 mL	0.9988 mL	1.9976 mL

 

产品信息

CAS号	955365-80-7
分子式	C2zH32N8O2
分子量	500.60
溶解度	DMSO	150.0 mg/mL (299.6 mM)
	Water	insoluble