Mefuparib hydrochloride (MPH) 是一种具有口服活性的，底物竞争性和选择性的 PARP1/2 抑制剂，IC₅₀ 分别为 3.2 nM 和 1.9 nM。Mefuparib hydrochloride 诱导细胞凋亡 (apoptosis)，并在体内外具有显着的抗癌活性。

Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC 50 s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo.

Solid

PARP1 3.2 nM (IC50) PARP2 1.9 nM (IC5

Mefuparib hydrochloride (1-10 μM; 48 hours) causes cell apoptosis.
Mefuparib hydrochloride (MPH; 1-10 μM; 24 hours) causes V-C8 cells into typical G2/M arrest.
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.
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).
Mefuparib hydrochloride inhibits PARP3 (IC50>10 μM), PARP6 (IC50>10 μM), TNKS1 (IC50=1.6 μM), TNKS2 (IC50=1.3 μM).
has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.
Mefuparib hydrochloride (10, 20, 40 mg/kg; oral) has a T 1/2 of 1.07-1.3 hours and a C max of 116-725 ng/mL for SD rats.
Mefuparib hydrochloride (5, 10, 20 mg/kg; oral) has a T 1/2 of 2.16-2.7 hours and a C max of 114-608 ng/mL for cynomolgus monkeys.
has not independently confirmed the accuracy of these methods. They are for refer

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: DMSO : 25 mg/mL (74.68 mM; Need ultrasonic)配制储备液