M3814 (nedisertib)

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5mg

￥1832.00

1648.00

- +
10mg

￥2822.00

2539.00

- +
25mg

￥5646.00

5081.00

- +
50mg

￥9114.00

8202.00

- +
100mg

￥14860.00

13374.00

- +

已选 0 种 0 瓶

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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.