China (Mainland)
Berzosertib (VE-822) CAS NO.1232416-25-9
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- Product Details
Keywords
- Berzosertib (VE-822)
- VX970, M6620
- 1232416-25-9
Quick Details
- ProName: Berzosertib (VE-822)
- CasNo: 1232416-25-9
- Molecular Formula: C24H25N5O3S
- ProductionCapacity: Metric Ton/Day
- Purity: >97%
- LimitNum: 0 Metric Ton
Superiority
Biological Activity
| Description | Berzosertib (VE-822, VX970, M6620) is an ATR inhibitor with IC50 of 19 nM in HT29 cells. | ||||||||||||||||||||||||||||||
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| Features | The first ATR-targeted drug candidate with high selectivity for ATR. | ||||||||||||||||||||||||||||||
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| In vitro |
VE-822 (80 nM) attenuates ATR signaling pathway and reduces survival in tumor cells in response to XRT and gemcitabine. VE-822 (80 nM) attenuates ATR signaling in normal cells without enhancing radiation and gemcitabine killing in normal cells. VE-822 (80 nM) increases XRT-induced residual γH2AX and 53BP1 foci compared with XRT in MiaPaCa-2 and PSN-1 cells. VE-822 (80 nM) pre-treatment decreases Rad51 foci after XRT in MiaPaCa-2 and PSN-1 cells. VE-822 (80 nM) alone increases the G1-phase-fraction in MiaPaCa-2 and PSN-1 cells. VE-822 (80 nM) abrogates XRT enriched G2/M-phase-fraction in MiaPaCa-2 and PSN-1 cells. VE-822 has little effect alone, while VE-822 (80 nM) combined with XRT and/or gemcitabine enhances early and late apoptosis in PSN-1 cells that is strongest in the triple combination. [1] VE-822 increases tumor response to DNA damaging agents associated with blockade of pChk1 Ser345. [2] |
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| In vivo | VE-822 (60 mg/kg) inhibits phospho-Ser-345-Chk1 in mice bearing PSN-1 tumors after DNA-damaging agents. VE-822 (60 mg/kg) combined with XTR doubles the time for tumors to grow to 600 mm3 of XRT alone in mice bearing both PSN-1 and MiaPaCa-2 tumors. VE-822 (60 mg/kg) added to the combination of gemcitabine and XRT substantially prolongs the tumor growth delay compared with the Gem+XRT1 group n mice bearing both PSN-1 tumors. VE-822 (60 mg/kg) combined with XRT1 increases uptake in tumors by 44% compared with XRT1, suggesting that addition of VE-822 increased γH2AX phosphorylation and persistence of DNA damage caused by XRT. [1] |