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Chemodex
MK-4827 tosylate
Product Details | |
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Synonyms | Niraparib tosylate; (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide 4 methylbenzenesulfonate |
Product Type | Chemical |
Properties | |
Formula | C19H20N4O . C7H8O3S |
MW | 492.6 |
CAS | 1038915-73-9 |
Source/Host Chemicals | Synthetic |
Purity Chemicals | ≥99% (HPLC) |
Appearance | White to off-white solid. |
Solubility | Soluble in DMSO or DMF (both 20mg/ml). Sparingly soluble in ethanol (1mg/ml) or water (<1mg/ml). |
Identity | Determined by 1H-NMR. |
Declaration | Manufactured by Chemodex. |
Other Product Data |
Click here for Original Manufacturer Product Datasheet |
InChi Key | LCPFHXWLJMNKNC-PFEQFJNWSA-N |
Smiles | NC(C1=CC=CC2=CN(C3=CC=C([C@H]4C[NH2+]CCC4)C=C3)N=C21)=O.CC5=CC=C(S(=O)([O-])=O)C=C5 |
Shipping and Handling | |
Shipping | AMBIENT |
Short Term Storage | +4°C |
Long Term Storage | -20°C |
Handling Advice | Protect from light and moisture. |
Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
Documents | |
MSDS | Inquire |
Product Specification Sheet | |
Datasheet | Download PDF |
MK-4827 is an orally bioavailable inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s=3.8 and 2.1nM, respectively). It inhibits the proliferation of cancer cells carrying the breast cancer mutations BRCA1 and BRCA2 in vitro and has efficacy alone against a xenograft of BRCA1-deficient cancer in mice. MK-4827 sensitizes human lung and breast cancer xenografts to radiation in mice.3 Formulations containing MK-4827 are effective against ovarian cancer.
(1) P. Jones, et al.; J. Med. Chem. 52, 7170 (2009) | (2) Y. Yuan, et al.; J. Hematol. Oncol. 4, 1 (2011) | (3) L. Wang, et al.; Invest. New Drugs 30, 2113 (2012) | (4) M.R. Mirza, et al.; N. Engl. J. Med. 375, 2154 (2016) | (5) K.N. Moore, et al.; Gynecol. Oncol. 149, 214 (2018) (Review)