VE 822
VE 822 Basic information
- Product Name:
- VE 822
- Synonyms:
-
- VX970 (VE-822)
- 2-Pyrazinamine, 3-[3-[4-[(methylamino)methyl]phenyl]-5-isoxazolyl]-5-[4-[(1-methylethyl)sulfonyl]phenyl]-
- VX970
- 3-[3-[4-[(Methylamino)methyl]phenyl]-5-isoxazolyl]-5-[4-[(1-methylethyl)sulfonyl]phenyl]-2-pyrazinamine VE-822
- VE 822 3-[3-[4-[(Methylamino)methyl]phenyl]-5-isoxazolyl]-5-[4-[(1-methylethyl)sulfonyl]phenyl]-2-pyrazinamine
- VE 822
- 3-[3-[4-[(Methylamino)methyl]phenyl]-5-isoxazolyl]-5-[4-[(1-methylethyl)sulfonyl]phenyl]-2-pyrazinamine
- VE822; VE 822
- CAS:
- 1232416-25-9
- MF:
- C24H25N5O3S
- MW:
- 463.55
- EINECS:
- 1592732-453-0
- Product Categories:
-
- Inhibitors
- Mol File:
- 1232416-25-9.mol
VE 822 Chemical Properties
- Melting point:
- >197°C (dec.)
- Boiling point:
- 674.4±55.0 °C(Predicted)
- Density
- 1.263±0.06 g/cm3(Predicted)
- storage temp.
- Refrigerator
- solubility
- DMSO (Slightly), Methanol (Slightly)
- pka
- 8.88±0.10(Predicted)
- form
- Solid
- color
- Light Yellow
VE 822 Usage And Synthesis
Uses
3-[3-[4-[(Methylamino)methyl]phenyl]-5-isoxazolyl]-5-[4-[(1-methylethyl)sulfonyl]phenyl]-2-pyrazinamine is a novel ATR (ATM-Rad3-related) inhibitor for in vitro and in vivo radiosensatization.
Definition
ChEBI: 3-[3-[4-(methylaminomethyl)phenyl]-5-isoxazolyl]-5-(4-propan-2-ylsulfonylphenyl)-2-pyrazinamine is a sulfonamide.
in vivo
PSN-1 xenografts are treated with Berzosertib (VE-822) (60 mk/kg; d0, 1), NSC 613327 (100 mg/kg; d0) and/or XRT (6 Gy; d1). Tumors are then harvested 2 h post-XRT. Berzosertib (VE-822) inhibits p-Ser-345-Chk1 in xenografts after DNA-damaging agents, establishing VE-822 as a potent inhibitor of ATR in vivo. Besides, Berzosertib (VE-822) enhances the therapeutic efficacy of radiation (XRT) in MiaPaCa-2 and PSN-1 xenograft models[1].
IC 50
ATR: 0.2 nM (Ki); ATM: 34 nM (Ki); PI3Kγ: 220 nM (Ki)
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