VE-822(Berzosertib), an analogue of VE-821 with increased potency and selectivity against ATR, increased solubility and good pharmacokinetic properties was shown to potently radiosensitise pancreatic cancer cell lines in vitro.VE-822 was the first selective ATR inhibitor to enter clinical development, and is now known as VX-970. In a recent study, published by Vertex Pharmaceuticals, VX-970 (VE-822) was shown to markedly sensitise a panel of non-small cell lung cancer cell lines, but not normal cells, to multiple DNA damaging drugs, namely cisplatin, oxaliplatin, gemcitabine, etoposide and SN38, the active metabolite of irinotecan.
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Name | VE-822 ( Berzosertib ) |
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Iupac Chemical Name | 5-(4-(isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine |
Synonyms | VE-822,VX-970;VE822;VE 822;Berzosertib; M6620; M-6620; M 6620; |
Molecular Formula | C24H25N5O3S |
Molecular Weight | 463.55 |
Smile | CNCC1=CC=C(C=C1)C1=NOC(=C1)C=1C(=NC=C(N1)C1=CC=C(C=C1)S(=O)(=O)C(C)C)N |
InChiKey | JZCWLJDSIRUGIN-UHFFFAOYSA-N |
InChi | InChI=1S/C24H25N5O3S/c1-15(2)33(30,31)19-10-8-18(9-11-19)21-14-27-24(25)23(28-21)22-12-20(29-32-22)17-6-4-16(5-7-17)13-26-3/h4-12,14-15,26H,13H2,1-3H3,(H2,25,27) |
CAS Number | 1232416-25-9 |
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Formulation | yellow solid |
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Purity | ≧98.0% |
Storage | 3 years -20ºCpowder |
Solubility | 5mg/ml in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. |
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Cell study | |
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Clinical study |