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KW-2478 819812-04-9

更新时间:2024-04-13

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简要描述:
KW-2478 819812-04-9
上海一基实业有限公司是主要从事配套试剂的生产和销售的企业,产品用途:科研实验,标准对照品研究中心代理的作为一种衡量标准

KW-2478 819812-04-9

KW2478
分子式:C30H42N2O9   分子量:574.66
 
产品描述
KW-2478 是非Ansamycin的HSP90抑制剂,IC50为3.8 nM。
靶点
HSP90
         
IC50
3.8 nM
         
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 and IGF-1Rβand c-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 for at least 12 hours is necessary to to exert potent antitumor activity. KW-2478 downregulates the translocation products of IgH locus. KW-2478 inhibits the transcription of c-Maf and cyclin D1 genes by mainly suppressing the function of Cdk9.KW-2478 has potent and 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 and 120-622 nM for B-cell lymphoma, mantle cell lymphoma and multiple myeloma, respectively. KW-2478 also shows potent growth inhibitory activity in primary CLL and NHL cells with EC50 of 40-170 nM and 200-400 nM, respectively.
体内研究
KW-2478 suppresses tumor growth and induces the degradation of client proteins in tumors in NCI-H929 s.c. inoculated model at doses of 100 mg/kg or more. KW-2478 reduces both serum M protein and MM tumor burden in the bone marrow in OPM-2/GFP i.v. inoculated mouse model at doses of 100 mg/kg.
溶解性
DMSO 115 mg/mL,水 <1 mg/mL,乙醇 3 mg/mL
稳定性
2年 -20°C粉状,6月-80°C溶于DMSO

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