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Niraparib hydrochloride

Cat. No. M13711
Niraparib hydrochloride Structure
Synonym:

MK-4827 hydrochloride

Size Price Availability Quantity
5mg USD 65  USD65 In stock
10mg USD 95  USD95 In stock
25mg USD 160  USD160 In stock
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Quality Control & Documentation
Biological Activity

Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.

Chemical Information
Molecular Weight 356.85
CAS Number 1038915-64-8
Solubility (25°C) DMSO 150 mg/mL
Water 90 mg/mL
Storage 2-8°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Arnold Lee. Target Oncol. Niraparib: A Review in First-Line Maintenance Therapy in Advanced Ovarian Cancer

[2] X H Wu, et al. Ann Oncol. Niraparib maintenance therapy in patients with platinum-sensitive recurrent ovarian cancer using an individualized starting dose (NORA): a randomized, double-blind, placebo-controlled phase III trial ☆

[3] Dea Slade. Genes Dev. PARP and PARG inhibitors in cancer treatment

[4] Antonio Gonzlez-Martn, et al. N Engl J Med. Niraparib in Patients with Newly Diagnosed Advanced Ovarian Cancer

[5] Mansoor R Mirza, et al. N Engl J Med. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer

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


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