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Devimistat (6,8-Bis(benzylthio)octanoic acid) 是一种线粒体代谢抑制剂,还是一种lipoic acid 拮抗剂,能阻断线粒体能量代谢,诱导多种癌细胞凋亡。
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Devimistat (6,8-Bis(benzylthio)octanoic acid) 是一种线粒体代谢抑制剂,还是一种lipoic acid 拮抗剂,能阻断线粒体能量代谢,诱导多种癌细胞凋亡。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 233 | 现货 | |
5 mg | ¥ 536 | 现货 | |
10 mg | ¥ 728 | 现货 | |
25 mg | ¥ 1,290 | 现货 | |
50 mg | ¥ 2,090 | 现货 | |
100 mg | ¥ 3,580 | 现货 | |
500 mg | ¥ 7,780 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 637 | 现货 |
产品描述 | Devimistat (6,8-Bis(benzylthio)octanoic acid) , a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts tumor cell mitochondrial metabolism. It has potential chemopreventive and antineoplastic activities, and has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Advanced Cancer, and Pancreatic Cancer, among others. |
体外活性 | 体外实验中,Devimistat 对包括H460人肺癌细胞和Saos-2人肉瘤细胞在内的多种肿瘤细胞线展现出选择性毒性,EC50均为120μM。Devimistat 干扰H460癌细胞的线粒体代谢,包括抑制PDH复合体活性以及以时间和化合物剂量依赖的方式导致线粒体膜电位丧失。此外,Devimistat (240μM)还能在H460人肺癌和Saos-2人肉瘤细胞中诱导凋亡和非凋亡细胞死亡。[1] |
体内活性 | Devimistat(25 mg/kg)在胰腺肿瘤细胞(BxPC-3)的人类肿瘤异种移植模型中显示出强大的抗癌活性。同样地,Devimistat(10 mg/kg)也在小鼠模型中显著抑制H460人类非小细胞肺癌的肿瘤生长。此外,Devimistat在大型动物模型中的预期治疗剂量范围内几乎不产生副作用毒性,而且在小鼠中的最大耐受剂量为100 mg/kg。[1] |
别名 | 辛酸, CPI-613, CPI613, CPI 613, 6,8-Bis(benzylthio)octanoic acid |
分子量 | 388.59 |
分子式 | C22H28O2S2 |
CAS No. | 95809-78-2 |
Smiles | OC(=O)CCCCC(CCSCc1ccccc1)SCc1ccccc1 |
密度 | 1.149 g/cm3 |
存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: 78 mg/mL (200.72 mM) DMSO: 45 mg/mL (115.8 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
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