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Mefuparib hydrochloride

产品编号 T11992 CAS 1449746-00-2

别名: 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

规格	价格/CNY	货期
2 mg	￥ 984	5日内发货
25 mg	￥ 6,860	10-14周
50 mg	￥ 8,920	10-14周
100 mg	￥ 13,800	10-14周

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其他形式的 Mefuparib hydrochloride:

Nectin-2 Protein, Mouse, Recombinant (His)
询价
Mefuparib Free Base
询价
Nectin-2 Protein, Human, Recombinant (His & Avi)
询价

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	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.
靶点活性	TNKS1:1.6 μM, PARP2:1.9 nM, PARP1:3.2 nM, TNKS2:1.3 μM
体外活性	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].
体内活性	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].

别名	MPH
分子量	334.77
分子式	C17H16ClFN2O2
CAS No.	1449746-00-2

存储

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

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参考文献

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.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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