A966492 Inhibitor CAS No. 934162-61-5

Cat. No.	Name	Size	Price
KI1243	A966492	5 mg	$272
	A966492	10 mg	$512
	A966492	50 mg	$1552
	A966492	200 mg	$3952

Chemical Characteristic

Product Name	A966492
CAS No.	934162-61-5
Molecular Weight	324.35
Formula	C₁₈H₁₇FN₄O
Chemical Name	2-[2-fluoro-4-[(2S)-pyrrolidin-2-yl]phenyl]-1H-benzimidazole-4-carboxamide
Smiles	c1(nc2c([nH]1)c(ccc2)C(=O)N)c1c(cc(cc1)C1NCCC1)F
Chemical Structure

Biological activities

A-966492 is a potent poly(ADP-Ribose) polymerase (PARP) inhibitor. The Ki of A-966492 is 1 and 1.5 nM against PARP1 and PARP2, respectively. A-966492 inhibits C41 whole cells with an EC50 of 1 nM.^[1] In a B16F10 subcutaneous murine melanoma model, A-966492 inhibits the growth of tumor. A-966492 significantly and dose-dependently enhances the antitumor efficacy of temozolomide. The combination of temozolomide with A-966492at the doses of 3, 10 and 30 mg/kg generates tumor growth inhibition by 35, 38 and 49%. In addition, in the B16 model, b.i.d dose of A-966492 (25 mg/kg/day) in combination with TMZ (50 mg/kg/day, qd) distributes tumors 6 hours after the final dose, with a concentration of 21 µg/mLin the tumor vs 0.38 µg/mL in the plasma. In a BRCA1-deficient MX-1 breast carcinoma model, A-966492, as well as the combination of carboplatin also inhibits the growth of tumor. ^[1]

References

[1] Penning TD, et al. Optimization of phenyl-substituted benzimidazolecarboxamidepoly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor. J Med Chem. 2010, 53(8): 3142-3153.

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