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编 号:F151075
分子式:C21H22N2O6S
分子量:430.47
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC50 of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues. PACMA 31 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

体内研究:
PACMA 31 (20 -200 mg/kg;腹腔注射;每日一次,持续 62 天) 抑制人卵巢癌小鼠异种移植物中的肿瘤生长。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.

体外研究:
PACMA 31 (0-10 μM;24 小时) 以剂量依赖性方式显著抑制 OVCAR-8 细胞的集落形成。
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