Gartisertib
| CAS号 | 1613191-99-3 | 货号 | BCP44100 |
| 中文名 | Gartisertib | ||
| 英文名 | Gartisertib | ||
| 中文别名 | |||
| 英文别名 | ATR inhibitor 2;M4344; M-4344; M 4344; VX-803; VX803; VX 803; Gartisertibum; | ||
| 分子式 | C25H29F2N9O3 | 分子量 | 541.55 |
| 生物活性 | Gartisertib is an orally available inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase, with potential antineoplastic activity. Upon oral administration, ATR kinase inhibitor VX-803 selectively inhibits ATR activity and blocks the downstream phosphorylation of the serine/threonine protein kinase CHK1. This prevents ATR-mediated signaling, which results in the inhibition of DNA damage checkpoint activation, the disruption of DNA damage repair, and the induction of tumor cell apoptosis. ATR, a serine/threonine protein kinase upregulated in a variety of cancer cell types, plays a key role in DNA repair, cell cycle progression and survival; it is activated by DNA damage caused during DNA replication-associated stress. | ||
| 信号通路 | Cell Cycle/DNA Damage | ||
| 靶 点 | ATM/ATR | ||
结构式
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