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。
CAS：1637542-33-6
分子式：C24H21ClFN5O3
分子量：481.91
纯度：98%
存储：Store at -20°C

Background:

Nedisertib (M3814) is a potent and selective inhibitor of DNA-dependent Protein Kinase (DNA-PK), with an IC50 of <3 nM.

Nedisertib (Compound 136) is a potent and selective inhibitor of DNA-PK, with an IC50 of <3 nM for DNA-PK and <0.5 μΜ for cellular pDNA-PK[3].

In combination with IR, Nedisertib shows efficacy in all of the 6 mouse models of human cancer. In all models, a dose of 2 Gy administered daily for 1 week in combination with Nedisertib induces statically significant tumor growth inhibition compare to IR alone. Nedisertib, alone or in combination with IR, does not induce significant weight loss or visual signs of toxicity in the mice in any study[1].

The efficacy of Nedisertib in combination with IR is evaluated in 6 human xenograft models (HCT116, FaDu, NCI-H460, A549, Capan-1, BxPC3) in mice representing 4 different cancer types (colon, head and neck, lung, and pancreas). Tumor cells are injected s.c. into nude mice, and treatment starts when palpable tumors are established (