MK-1775 | CAS:955365-80-7

Chemscene社は、高品質な低分子化合物を提供しているメーカーです。
Chemscene社のMK-1775(CAS:955365-80-7)をご紹介します。

※本製品は研究用です。研究用以外には使用できません。

Name:MK-1775; AZD1775; Adavosertib
Cat. No. :CS-0105
CAS No. :955365-80-7
Formula:C27H32N8O2
M. Wt. : 500.60
Solubility:10 mM in DMSO

MK-1775 is a potent Wee1 inhibitor with IC50 of 5.2 nM.IC50 & Target: IC50: 5.2 nM (Wee1)In Vitro: MK-1775 enhances the cytotoxic effects of 5-FU in p53-deficient human colon cancer cells. MK-1775 inhibits CDC2 Y15 phosphorylation in cells, abrogates DNA damaged checkpoints induced by 5-FU treatment, and causes premature entry of mitosis determined by induction of Histone H3 phosphorylation[1]. MK-1775 abrogates the radiation-induced G2 block in p53-defective cells but not in p53 wild-type lines[2]. The combination of gemcitabine with MK-1775 produces robust anti-tumor activity and remarkably enhances tumor regression response (4.01 fold) compared to gemcitabine treatment in p53-deficient tumors[3]. In Vivo: In vivo, MK-1775 potentiates the anti-tumor efficacy of 5-FU or its prodrug, capecitabine, at tolerable doses[1]. MK-1775 (60 mg/kg twice daily, p.o.) enhances H1299 xenograft tumor response to fractionated radiotherapy[2]. MK-1775 (30 mg/kg. p.o.) regresses tumor growth in PANC198, PANC215 and PANC185 as compared to GEM treated mice[3].

Rajeshkumar NV, et al. MK-1775, a potent Wee1 inhibitor, synergizes with gemcitabine to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts.Clin Cancer Res. 2011 May 1;17(9):2799-806. Epub 2011 Mar 9. Bridges KA, et al. MK-1775, a novel Wee1 kinase inhibitor, radiosensitizes p53-defective human tumor cells. Clin Cancer Res. 2011 Sep 1;17(17):5638-48. Epub 2011 Jul 28. Hirai H, et al. MK-1775, a small molecule Wee1 inhibitor, enhances anti-tumor efficacy of various DNA-damaging agents, including 5-fluorouracil Cancer Biol Ther. 2010 Apr;9(7):514-22.