Chemodex

MK-4827 tosylate

CHF 217.00
In stock
CDX-M0565-M01010 mgCHF 217.00
CDX-M0565-M05050 mgCHF 474.00
More Information
Product Details
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
Our product description may differ slightly from the original manufacturers 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
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Product Specification Sheet
Datasheet Download PDF
Description

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.

Product References

(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)

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