PACMA 31

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PACMA 31 是一种不可逆的蛋白质二硫键异构酶 (PDI) 共价抑制剂，IC50 为 10 μM。 PACMA 31 显着抑制卵巢肿瘤生长并表现出肿瘤靶向能力。

PACMA 31 is an irreversible and covalent inhibitor of protein disulfide isomerase (PDI) with an IC50 of 10 μM. PACMA 31 significantly suppresses ovarian tumor growth and exhibits tumor targeting ability.(In Vitro):In OVCAR-8 cells, PACMA 31 (0-10 μM) potently inhibits colony formation in a dose-dependent manner.(In Vivo):In human ovarian cancer mouse xenografts, PACMA 31 (20-200 mg/kg) i.p. or per os administration of significantly inhibited tumor growth by 85% and 65% at day 62, respectively.

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Animal Model:Athymic mice (bearing OVCAR-8 cells)Dosage:20-200 mg/kg Administration:I.p., per day for the first 3 wk with 5-d on and 2-d off treatment cycles, and dose was escalated to 40 mg/kg per day for the next 7 d; p.o., the initial dose of 20 mg/kg per day was gradually increased by 20 mg/kg per day with each dose for 3 d before it was orally dosed at 200 mg/kg per day for an additional 32 d, increasing the dose from 20 to 200 mg/kg Result:Compared with the control group, i.p. or per os administration of PACMA 31 significantly inhibited tumor growth by 85% and 65% at day 62, respectively.

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Others

Other Targets

P-gp

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1401089-31-3

430.47

C21H22N2O6S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (232.30 mM)

O=C(C#C)N(C1=CC=C(OC)C=C1OC)C(C(=O)NCC(=O)OCC)C=2SC=CC2

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(-20℃)

With Ice Pack

≥ 2 years