Gartisertib
| CAS No. | 1613191-99-3 | Cat. No. | BCP44100 |
| Name | Gartisertib | ||
| Synonyms | ATR inhibitor 2;M4344; M-4344; M 4344; VX-803; VX803; VX 803; Gartisertibum; | ||
| Formula | C25H29F2N9O3 | M. Wt | 541.55 |
| Description | 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. | ||
| Pathways | Cell Cycle/DNA Damage | ||
| Targets | ATM/ATR | ||
Structure
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