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|Product Name:||Niraparib||Other Name:||MK-4827|
|Packaging:||Foil Bag Or Vial||Form:||Powder|
|Assays:||99%||Shipping:||By Express (FedEx,UPS,DHL,EMS), By Air And By Sea|
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selective androgen receptor modulators
Niraparib (also known as MK-4827) is a potent, orally bioavailable and selective inhibitor of PARP1/2 with IC50 of 3.8 nM and 2.1nM for PARP 1 and 2 respectively. Niraparib is approved by the US FDA on 27 March 2017 for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in complete or partial response to platinum-based chemotherapy. Niraparib demonstrated high activity in cancer cells with mutant BRCA-1 and BRCA-2 with IC50 in the 10−100 nM range. It is >330-fold selective against PARP3, V-PARP and Tank1. In a whole cell assay, MK-4827 inhibited PARP activity with EC50 of 4 nM. MK-4827 also inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. MK-4827 strongly enhanced the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant.
CAS No.: 1038915-60-4
Other Names: Niraparib
EINECS No.: 1038915-60-4
Place of Origin: Shanghai, China (Mainland)
Type: Antineoplastic Agents
Grade Standard: Medicine Grade
Usage: Animal Pharmaceuticals
Brand Name: TwoChem
Model Number: API
Appearance: Off-White Powder
Grade: Phamaceutical Grade
Application: Active Pharmaceutical Ingredients
Niraparib (MK-4827), a new, potent andorally available PARP-1 and PARP-2 inhibitor, is currently in phase IIIclinical trials for the treatment of ovarian cancer and phase III trials areplanned to begin for breast cancer.
The drug is used in form of the salt niraparib tosylate monohydrate, which is white to off-white, non-hygroscopic crystals
The drug is approved by the US FDA for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in complete or partial response to platinum-based chemotherapy.
In a study with 553 patients, progression-free survival (PFS) for patients with a deleterious or suspected deleterious BRCA mutation in the germline was 21.0 months under niraparib therapy, as compared to 5.5 months under placebo. Patients without such a mutation had a PFS of 9.3 months under niraparib versus 3.9 months under placebo.
The most common side effects in studies were low blood cell counts, namely thrombocytopenia (in 61% of patients, severe in 29%), anemia (in 50%, severe in 25%) and neutropenia (in 30%, severe in 20%). Other, mostly mild to moderate side effects included nausea, fatigue, and constipation. In a study running over 250 days (median), 15% of patients had to permanently discontinue niraparib due to adverse effects.
|Molecular Weight (MW)||320.39|
|CAS No.||1038915-60-4 (free base); 1038915-73-9 (tosylate); 1038915-64-8 (HCl); 1613220-15-7 (tosylate hydrate); 1476777-06-6 (Niraparib metabolite M1); 1038915-58-0 (Niraparib R-enantiomer)|
|Storage||-20℃ for 3 years in powder form|
|-80℃ for 2 years in solvent|
|Solubility (In vitro)||DMSO: 64 mg/mL (199.8 mM)|
|Water: <1 mg/mL|
|Ethanol: 64 mg/mL (199.8 mM)|
|Synonyms||MK-4827; MK 4827; MK4827; Niraparib. Niraparib free base|
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