| 货号 | 4701/10 |
| 别名 | 5-[2-Amino-4-chloro-7-[(4-methoxy-3 |
| 供应商 | Tocris |
| 生物活性 | High affinity, potent and selective Hsp90 inhibitor (Ki = 0.2 nM and IC50 = 1.1 nM). Exhibits selectivity for Hsp90 over Grp94 and TRAP1 (Ki values are 61 and 255 nM respectively) and has no effect (IC50>10μM) against a panel of 285 kinases. Degrades Her-2 in MCF-7 breast cancer cells (EC50 = 14 nM). Blocks tumor growth and induces partial tumor regression in an N87 gastric tumor mouse model. Also inhibits LPS-induced TNFα release in an LPS shock mouse model and suppresses disease development in a rat model of collagen-induced arthritis. Exhibits <20-fold efficacy over BIIB 021 (Cat. No. 4608) in mice. Orally available and brain penetrant. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >98 % |
| 计算分子量 | 413.9 |
| 分子式 | C21H24ClN5O2 |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO |
| 参考文献 | Shiet al (2012) EC144 is a potent inhibitor of the heat shock protein 90. J.Med.Chem. 55 7786. PMID: 22938030. Yunet al (2011) EC144, a synthetic inhibitor of heat shock protein 90, blocks innate and adaptive immune responses in models of inflammation and autoimmunity. J.Immunol. 186 563. PMID: 21131419. |