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Chemical Structure : Simmiparib
CAS No.: 1551355-46-4
Catalog No.: PC-61950Not For Human Use, Lab Use Only.
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).
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|---|---|---|---|
| 5 mg | $298 | In stock | |
| 10 mg | $488 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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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).
Simmiparib selectively induces the accumulation of DNA double-strand breaks, G2/M arrest and apoptosis in homologous recombination repair (HR)-deficient cells.
Simmiparib potentiates the proliferative inhibition of several conventional anticancer drugs, reduces the poly(ADP-ribose) formation in HR-deficient cancer cells and xenografts.
Simmiparib exhibits 10-fold greater growth inhibition than olaparib against HR-deficient human cancer cell- or tissue-derived xenografts in nude mice.
| M.Wt | 486.431 | |
| Formula | C23H18F4N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-(4-fluoro-3-(5-methyl-3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)benzyl)phthalazin-1(2H)-one |
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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.
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