PACMA 31
目录号: PL09500 纯度: ≥99%
CAS No. :1401089-31-3
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PL09500-5mg 5mg ¥1085.00 请登录
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中文名称
PACMA 31
中文别名
PACMA 31
英文名称
PACMA 31
英文别名
PACMA 31;N-(2,4-Dimethoxyphenyl)-N-(1-oxo-2-propyn-1-yl)-2-(2-thienyl)glycyl-glycine ethyl ester;PACMA 31, >=98% (HPLC);N-(2,4-Dimethoxyphenyl)-N-(1-oxo-2-propyn-1-yl)-2-(2-thienyl)glycylglycineethylester;N-(2,4-Dimethoxyphenyl)-N-(1-oxo-2-propyn-1-yl)-2-(2-thienyl)glycylglycine ethyl ester;Ethyl 2-[[2-(2,4-dimethoxy-N-prop-2-ynoylanilino)-2-thiophen-2-ylacetyl]amino]acetate
Cas No.
1401089-31-3
分子式
C21H22N2O6S
分子量
430.47
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
PACMA 31 是一种不可逆的口服活性蛋白二硫化物异构酶 (PDI) 抑制剂,IC50 为 10μM,PACMA 31 与 PDI 的活性部位半胱氨酸形成共价键。PACMA 31 具有肿瘤靶向性,能显著抑制卵巢肿瘤生长,对正常组织无毒性。
生物活性
PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC 50 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.
性状
Solid
IC50 & Target[1][2]
IC50: 10 μM (protein disulfide isomerase)
体外研究(In Vitro)
PACMA 31 (0-10 μM; 24 hours) significantly inhibits colony formation in OVCAR-8 cells in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
PACMA 31 (20-200 mg/kg; i.p.; daily for 62 days) suppresses tumor growth in human ovarian cancer mouse xenografts . has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Athymic mice (beari
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Xu S, et al. Discovery of an orally active small-molecule irreversible inhibitor of protein disulfide isomerase for ovarian cancer treatment. Proc Natl Acad Sci U S A. 2012;109(40):16348-16353.
溶解度数据
In Vitro: DMSO : 100 mg/mL (232.30 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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