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KI1219MK-482710 mg$670

Chemical Characteristic

Product NameMK-4827
CAS No.1038915-64-8
Molecular Weight 320.39
FormulaC19H20N4O
Chemical Name(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide
Smilesn1n(cc2cccc(c12)C(=O)N)c1ccc(cc1)C1CNCCC1
Chemical Structure

Biological activities

MK-4827 is a potent, selective inhibitor of PARP1 and PARP2 with IC50 of 3.8 and 2.1 nM, respectively. MK-4827 also shows at least a 100-fold selectivity over PARP-3, V-PARP, and TANK-1, with IC50 values of 1300, 330, and 570 nM, respectively. In MDA-MB-436 human mammary gland adenocarcinoma cells carrying BRCA-1mutations, and CAPAN-1 human pancreatic adenocarcinoma cells carrying BRCA-2 mutant, MK-4827 displays CC50 value of 18 and 90 nM, respectively. However, normal human prostate and mammary epithelial cells are resistant to MK-4827, displaying antiproliferative effects in the micromolar range. In a BRCA-1 mutant MDA-MB-436 xenograft model, MK-4827 treatment (100 mg/kg q.d. or 50 mg/kg b.i.d.) achieves significant tumor regression with no mortality.[1] In Calu-6 (p53 null), A549 (p53 wild-type) and H-460 (p53 wt) lung cancers and triple negative MDA-MB-231 human breast carcinoma xenografts of differing p53 status, combined treatment efficacy of MK-4827 (50 mg/kg once daily or 25 mg/kg twice daily) and fractionated radiotherapy radiosensitizes all four tumors studied regardless of their p53 status.[2]

Protocols

In vitro: MK-4827 is dissolved in 5%DMSO/H2O.[1]

References

[1] Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7- carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009, 52(22): 7170-7185.
[2] Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012, 30(6): 2113-2120.

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