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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-DNA-PK-M3814
M3814

Chemical Structure : M3814

CAS No.: 1637542-33-6

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M3814 (Peposertib; Nedisertib; M 3814; MSC2490484A)

货号: PC-61389Not For Human Use, Lab Use Only.

M3814 (Nedisertib, Peposertib, MSC2490484A) is a highly potent, selective, ATP-competitive and orally bioavailable inhibitor of DNA-PK with IC50 of 0.6 nM (10 uM ATP).

规格 价格 库存 数量
5 mg ￥1480 In stock
10 mg ￥2280 In stock
25 mg ￥3980 In stock
50 mg ￥5980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

M3814 (Nedisertib, Peposertib, MSC2490484A) is a highly potent, selective, ATP-competitive and orally bioavailable inhibitor of DNA-PK with IC50 of 0.6 nM (10 uM ATP).
M3814 exhibited a high degree of selectivity when tested using a broad panel of serine/threonine, tyrosine, and lipid kinases, only 8of 284 recombinantly expressed protein/lipid kinases, including mutant kinases, were inhibited by at least 50% at 1 μmol/L M3814.
M3814 selectively inhibits DNA-PK activity and DSB repair in human cancer cell lines.
M3814 sensitizes cancer cells to IR through impaired colony outgrowth or proliferation/viability.
M3814 inhibits radiation-induced DNA-PK autophosphorylation and DSB repair in tumor xenograft models.
M3814 in combination with ionizing radiation (IR) has antitumor activity in mouse xenograft models.

物理化学性质&存储条件

分子量 481.912
分子式 C24H21ClFN5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-{2-chloro-4-fluoro-5-[7-(morpholin-4-yl)quinazolin-4-yl]phenyl}(6-methoxypyridazin-3-yl)methanol

参考文献

1. Harnor SJ, et al. ChemMedChem. 2017 Jun 21;12(12):895-900.
2. Zenke FT, et al. Mol Cancer Ther. 2020 May;19(5):1091-1101.

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