用途
KW-2478 |
参数 | 数值 |
生物活性 | KW-2478是一种非Ansamycin的HSP90抑制剂,IC50为3.8 nM。Phase 1。 | 体外研究 | KW-2478 inhibits the binding of bRD to Hsp90α with IC50 of 3.8 nM. KW-2478 degradates the Hsp90 client proteins, including FGFR3 IGF-1Rβc-Raf-1. KW-2478 reduces the level of phosphorylated Erk1/2. KW-2478 induces apoptosis by cleavage of PARP, a substrate of caspase-3 In U266 cells,. KW-2478 has Time dependency of antiproliferative activity, consecutive drug exposure fat least 12 hours is necessary to to exert potent antitumactivity. KW-2478 downregulates the translocation products of IgH locus. KW-2478 inhibits the transcription of c-Maf cyclin D1 genes by mainly suppressing the function of Cdk9. KW-2478 has potent broad growth inhibitory activities against various cell lines, KW-2478 inhibites cancer cell growth in all cell lines, with EC50 of 101-252 nM, 81.4-91.4 nM 120-622 nM fB-cell lymphoma, mantle cell lymphoma multiple myeloma, respectively. KW-2478 also shows potent growth inhibitory activity in primary CLL NHL cells with EC50 of 40-170 nM 200-400 nM, respectively. . | 体内研究 | KW-2478 suppresses tumgrowth induces the degradation of client proteins in tumors in NCI-H929 s.c. inoculated model at doses of 100 mg/kg more. KW-2478 reduces both serum M protein MM tumburden in the bone marrow in OPM-2/GFP i.v. inoculated mouse model at doses of 100 mg/kg. | 别名 | 2-乙基-3,5-二羟基-N,N-双(2-甲氧基乙基)-6-[3-甲氧基-4-[2-(4-吗啉基)乙氧基]苯甲酰基]苯乙酰胺 | 英文别名 | KW-2478;2-Ethyl-3,5-dihydroxy-N,N-bis(2-methoxyethyl)-6-[3-methoxy-4-[2-(4-morpholinyl)ethoxy]benzoyl]benzeneacetamide;2-(2-ethyl-3,5-dihydroxy-6-(3-methoxy-4-(2-morpholinoethoxy)benzoyl)phenyl)-N,N-bis(2-methoxyethyl)acetamide;2-Ethyl-3,5-dihydroxy-N,N-bis(2-methoxyethyl)-6-[3-methoxy-4-[2-(4-morpholinyl)ethoxy]benzoyl]benzeneacetamideKW2478;2-(2-Ethyl-3,5-dihydroxy-6-(3-methoxy-4-(2-morpholinoethoxy)benzoyl)phenyl)-N,N-bis(2-methoxye | |
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供应 819812-04-9 | 供应 KW-2478 | 现货 819812-04-9 | 现货 KW-2478 | 高纯 819812-04-9 | 高纯 KW-2478 | 定制 819812-04-9 | 定制 KW-2478 | 819812-04-9 供应商 | KW-2478 供应商 | 819812-04-9 生产厂家 | KW-2478 生产厂家 | 819812-04-9 价格 | KW-2478 价格 | 819812-04-9 现货 | KW-2478 现货 | 819812-04-9 作用 | KW-2478 作用 | 819812-04-9 原料 | KW-2478 原料 | 819812-04-9 定制 | KW-2478 定制 | 819812-04-9 试剂 | KW-2478 试剂 |
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