M3814是一个有效且有选择性的DNA依赖性蛋白激酶(DNA-PK)的抑制剂。
货号：ajce49678
CAS：1637542-33-6
分子式：C24H21ClFN5O3
分子量：481.91
纯度：98%
存储：Store at -20°C
库存：现货
Background:
Nedisertib (M3814, Peposertib, MSC2490484A) is an orally bioavailable, highly potent and selective inhibitor of DNA activated protein kinase (DNA-PK) with IC50 of < 3 nM.
M3814 potently inhibits DNA-PK catalytic activity and sensitizes multiple cancer cell lines to ionizing radiation (IR) and DSB-inducing agents. Inhibition of DNA-PK autophosphorylation in cancer cells leads to an increased number of persistent DSBs.[2]
Inhibition of DNA-PK autophosphorylation in xenograft tumors leads to an increased number of persistent DSBs. Oral administration of M3814 to two xenograft models of human cancer, using a clinically established 6-week fractionated radiation schedule, strongly potentiates the antitumor activity of IR and lead to complete tumor regression at nontoxic doses.[2]
参考文献：
[1] Thomas Fuchss, et al. WO2014183850A1.
[2] Frank T Zenke, et al. Mol Cancer Ther. 2020 May;19(5):1091-1101.
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