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Mefuparib hydrochloride

Catalog No. T11992   CAS 1449746-00-2
Synonyms: MPH

Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo. Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively.

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Mefuparib hydrochloride Chemical Structure
Mefuparib hydrochloride, CAS 1449746-00-2
Pack Size Availability Price/USD Quantity
25 mg 10-14 weeks $ 668.00
50 mg 10-14 weeks $ 868.00
100 mg 10-14 weeks $ 1,310.00
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Biological Description
Chemical Properties
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Description Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo. Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively.
Targets&IC50 TNKS1:1.6 μM, PARP2:1.9 nM, PARP1:3.2 nM, TNKS2:1.3 μM
In vitro Mefuparib hydrochloride (1-10 μM; 24 hours) causes the accumulation of DSB marked by the increased levels of γH2AX in the MDA-MB-436 (BRCA1?/?) cells in a concentration-dependent manner[1]. Mefuparib hydrochloride exerts potent in vitro proliferation-inhibitory effects on cancer cells derived from different human tissues with an average IC50 of 2.16 μM (0.12 μM~3.64 μM)[1]. Mefuparib hydrochloride inhibits PARP3 (IC50>10 μM), PARP6 (IC50>10 μM), TNKS1 (IC50=1.6 μM), TNKS2 (IC50=1.3 μM)[1].Mefuparib hydrochloride (1-10 μM;?48 hours) causes cell apoptosis[1].??Mefuparib hydrochloride (MPH;?1-10 μM;?24 hours) causes V-C8 cells into typical G2/M arrest[1].
In vivo Mefuparib hydrochloride (10, 20, 40 mg/kg; oral) has a T1/2 of 1.07-1.3 hours and a C max of 116-725 ng/mL for SD rats[1]. Mefuparib hydrochloride (5, 10, 20 mg/kg; oral) has a T1/2 of 2.16-2.7 hours and a C max of 114-608 ng/mL for cynomolgus monkeys[1].?Mefuparib hydrochloride (MPH;?40-160 mg/kg;?orally;?once every other day;?for 21 days) displays dose- and time-dependent killing on V-C8 xenografts accompanied by complete disappearance of some xenografts, especially in the high-dose group[1].??Mefuparib hydrochloride (160 mg/kg;?orally;?once every other day;?for 21 days) inhibits the growth of the BR-05-0028 breast patient-derived xenograft (PDX) without obvious loss of body weight[1].
Synonyms MPH
Molecular Weight 334.77
Formula C17H16ClFN2O2
CAS No. 1449746-00-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. He JX, et al. Novel PARP1/2 inhibitor mefuparib hydrochloride elicits potent in vitro and in vivo anticancer activity, characteristic of high tissue distribution. Oncotarget. 2017 Jan 17;8(3):4156-4168. 2. Nie D, et al. Cancer-Cell-Membrane-Coated Nanoparticles with a Yolk-Shell Structure Augment Cancer Chemotherapy. Nano Lett. 2020 Feb 12;20(2):936-946.

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Keywords

Mefuparib hydrochloride 1449746-00-2 Chromatin/Epigenetic DNA Damage/DNA Repair PARP MPH Mefuparib Hydrochloride inhibitor inhibit

 

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