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Signaling Pathway

MK-4827

HY-10619

(Niraparib; MK 4827; MK4827)

MK-4827

MK-4827 Chemical Structure

MK-4827(Niraparib) is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM; with great activity in cancer cells with mutant BRCA-1 and BRCA-2; >330-fold selective against PARP3, V-PARP and Tank1.

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Free sample   Apply now  
10 mM * 1 mL in DMSO $132 In-stock
5 mg $120 In-stock
10 mg $200 In-stock
50 mg $600 In-stock
100 mg $1000 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €129 In-stock
5 mg €118 In-stock
10 mg €196 In-stock
50 mg €588 In-stock
100 mg €980 In-stock
200 mg Get quote
500 mg Get quote

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Product name: MK-4827
Cat. No.: HY-10619

MK-4827 Data Sheet

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    Purity: 99.39% ee.:99.90%

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    DataSheet

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Biological Activity of MK-4827

MK-4827(Niraparib) is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM; with great activity in cancer cells with mutant BRCA-1 and BRCA-2; >330-fold selective against PARP3, V-PARP and Tank1.
IC50 value: 3.8 nM/2.1 nM( PARP1/2) [1]
Target: PARP1/2
in vitro: MK-4827 displays excellent PARP 1 and 2 inhibition with IC(50) = 3.8 and 2.1 nM, respectively, and in a whole cell assay, it inhibits PARP activity with EC(50) = 4 nM and inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC(50) in the 10-100 nM range [1].
in vivo: MK-4827 is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer [1]. In addition, MK-4827 strongly enhances the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant. The enhancement of radiation response is observed in clinically relevant radiation-dose fractionation schedules. The therapeutic window during which time MK-4827 interacts with radiation lasts for several hours. These biological attributes make translation of this therapeutic combination treatment feasible for translation to the treatment of a variety of human cancers [2].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 320.39 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C19H20N4O
CAS No 1038915-60-4
Solvent & Solubility

DMSO: ≥ 34 mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 3.1212 mL 15.6060 mL 31.2120 mL
5 mM 0.6242 mL 3.1212 mL 6.2424 mL
10 mM 0.3121 mL 1.5606 mL 3.1212 mL

Clinical Information of MK-4827

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
MK-4827 Merck & Co Inc Mantle cell lymphoma 31-DEC-10 01-AUG-13 Phase 2 13-SEP-13
TESARO Inc Metastatic breast cancer 31-OCT-13 31-OCT-15 Phase 3 20-NOV-13
TESARO Inc Fallopian tube cancer 30-JUN-13 31-MAR-16 Phase 3 30-AUG-13
Merck & Co Inc Glioblastoma 28-FEB-11 31-MAY-12 Phase 1 16-AUG-12
Merck & Co Inc Ovary tumor 30-NOV-10 30-SEP-11 Phase 1 20-MAR-12
TESARO Inc Peritoneal tumor 30-JUN-13 31-MAR-16 Phase 3 30-AUG-13

References on MK-4827

Other Forms

Inhibitor Kit

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