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M6620

Chemical Structure : M6620

CAS No.: 1232416-25-9

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

Catalog No.: PC-72164Not For Human Use, Lab Use Only.

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

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100 mg $898 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

M6620 (Berzosertib, 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.

Physicochemical Properties

M.Wt 463.556
Formula C24H25N5O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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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