Free shipping on all orders over $ 500

MK-4827

Cat. No. M2215
MK-4827 Structure
Synonym:

Niraparib

Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 210 In stock
50mg USD 400 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

MK-4827 (Niraparib) is an oral potent, selective PARP-1 and PARP-2 inhibitor currently in phase I clinical trials for cancer treatment. MK-4827 shows excellent PARP 1 and 2 inhibition with IC(50) = 3.8 and 2.1 nM, respectively, and in a whole cell assay, it inhibited PARP activity with EC(50) = 4 nM and inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC(50) in the 10-100 nM range. MK-4827 reduced PAR levels in tumors by 1 h after administration which persisted for up to 24 h. MK-4827 was well tolerated in vivo and demonstrated efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. In addition, MK-4827 strongly enhances the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 320.39
Formula C19H20N4O
CAS Number 1038915-60-4
Purity >99%
Solubility DMSO
Storage at -20°C
References

The poly(ADP-ribose) polymerase inhibitor niraparib (MK4827) in BRCA mutation carriers and patients with sporadic cancer: a phase 1 dose-escalation trial.
Sandhu SK, et al. Lancet Oncol. 2013 Aug;14(9):882-92. PMID: 23810788.

MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation.
Wang L, et al. Invest New Drugs. 2012 Dec;30(6):2113-20. PMID: 22127459.

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.
Jones P, et al. J Med Chem. 2009 Nov 26;52(22):7170-85. PMID: 19873981.

Related PARP Products
Daidzein

Daidzein is an inactive analogue of genistein, a tyrosine kinase inhibitor and an estrogen receptor activator.

NMS-P118

NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively).

E7449

E7449 is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 that also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively.

BMN673 isomer

BMN-673 8R,9S

BMN-673 (8R,9S) is the (8R,9S) enantiomer of BMN-673.BMN673 is a potent inhibitor of poly (ADP-ribose) polymerases (PARP)-1 and -2.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MK-4827, Niraparib supplier, PARP, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.