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Chemical Structure : Berzosertib
CAS No.: 1232416-25-9
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $78 | In stock | |
| 10 mg | $118 | In stock | |
| 50 mg | $278 | In stock | |
| 100 mg | $458 | In stock | |
| 250 mg | Get quote |
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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.
| M.Wt | 463.556 | |
| Formula | C24H25N5O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine |
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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.
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