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Simmiparib

Names

[ CAS No. ]:
1551355-46-4

[ Name ]:
Simmiparib

Biological Activity

[Description]:

Simmiparib is a novel potent, orally active PARP1/2 inhibitor with IC50 of 1.75/0.22 nM, inhibits PARP1 >90-fold more potently than the other PARPs (PARP3, TNKS1, TNKS2); selectively induces the accumulation of DNA double-strand breaks, G2/M arrest and apoptosis in homologous recombination repair (HR)-deficient cells; potentiates the proliferative inhibition of several conventional anticancer drugs, reduces the poly(ADP-ribose) formation in HR-deficient cancer cells and xenografts; exhibits 10-fold greater growth inhibition than olaparib against HR-deficient human cancer cell- or tissue-derived xenografts in nude mice. Solid Tumors Phase 1 Clinical

[References]

References 1. Yuan B, et al. Cancer Lett. 2017 Feb 1;386:47-56. 2. Yang ZM, et al. Acta Pharmacol Sin. 2017 Jul;38(7):1038-1047. View Related Products by Target PARP Solid Tumors

Chemical & Physical Properties

[ Molecular Formula ]:
C23H18F4N6O2

[ Molecular Weight ]:
486.431


Related Compounds