Berzosertib (M6620, VX-970, VE-822)

Chemical Structure : Berzosertib

CAS No.: 1232416-25-9

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货号: PC-72164Not For Human Use, Lab Use Only.

Berzosertib (M6620, VX-970, VE-822) is a highly potent, selective ATR inhibitor with Ki of 0.17 nM, pH2AX IC50 of 19 nM.

规格	价格	库存
5 mg	￥780	In stock
10 mg	￥1180	In stock
50 mg	￥2780	In stock
100 mg	￥4580	In stock
250 mg		Get quote

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生物&药学活性

Berzosertib (M6620, VX-970, VE-822) is a highly potent, selective ATR inhibitor with Ki of 0.17 nM, pH2AX IC50 of 19 nM.
M6620 (Berzosertib, VX-970) displays >250-fold selectivity over ATM, and no inhibition against DNA-PK, 278 out of 291 kinases showed <50% inhibition at 400 nM, only Flt4 kinase shows less than 100-fold selectivity.
M6620 (Berzosertib, VX-970) preferentially inhibited ATR-Chk1-CDC25a signaling, abrogated the radiotherapy-induced G2-M checkpoint, delayed resolution of DNA double-strand breaks, and reduced colony formation after radiotherapy in TNBC cells relative to normal-like breast epithelial cells.
M6620 (Berzosertib, VX-970) demonstrated durable regressions in small cell lung cancers with high replication stress when combined with TOP1 inhibitor topotecan.

物理化学性质&存储条件

分子量	463.556
分子式	C24H25N5O3S
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	5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine

参考文献

1. Gorecki L, et al. Pharmacol Ther. 2020 Jun;210:107518.

2. Knegtel R, et al. J Med Chem. 2019 Jun 13;62(11):5547-5561.

3. Tu X, et al. Mol Cancer Ther. 2018 Nov;17(11):2462-2472.

4. Thomas A, et al. J Clin Oncol. 2018 Jun 1;36(16):1594-1602.