Mefuparib盐酸美呋哌瑞,1449746-00-2

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Mefuparib hydrochloride

CAS No. : 1449746-00-2

MCE 国际站：Mefuparib hydrochloride

产品活性：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。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Apoptosis

作用靶点：PARP  |  Apoptosis

In Vitro: 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).

In Vivo: 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.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  Epigenetics Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Children’s Drug Library  |  Heterocyclic Compound Library  |  Highly Selective Inhibitors Library  |  Highly Selective Activators Library  |  Cell Death Library  |  MG-132  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Olaparib  |  LY294002  |  Tamoxifen  |  Paclitaxel  |  Y-27632  |  Acetylcysteine  |  Angiotensin II human  |  2-Deoxy-D-glucose  |  Staurosporine  |  SB-431542  |  Actinomycin D  |  Deferoxamine mesylate  |  Bortezomib  |  5-Fluorouracil  |  Trametinib  |  Sorafenib  |  Oxaliplatin  |  Gemcitabine  |  Temozolomide  |  Rotenone  |  Mdivi-1  |  Elesclomol  |  Ruxolitinib  |  Decitabine  |  SP600125  |  MK-2206 dihydrochloride  |  Etoposide

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds