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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; | ||
SMILES | C1CN(CCC1C(=O)N2CCN(CC2)C3COC3)C4=C(C=NC=C4NC(=O)C5=C6N=CC(=CN6N=C5N)F)F | ||
Chemical Name | |||
Formula | C25H29F2N9O3 | M. Wt | 541.55 |
Purity | 98% | Storage | Store at 4-8°C |
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. |
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