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KW-2478 {[allProObj[0].p_purity_real_show]}

货号:A554986

KW-2478是一种非缬氨酸类 HSP90 抑制剂,IC50 为 3.8 nM,具有抗肿瘤活性,尤其在血液肿瘤细胞中表现显著。

KW-2478 化学结构 CAS号:819812-04-9
KW-2478 化学结构
CAS号:819812-04-9
KW-2478 3D分子结构
CAS号:819812-04-9
KW-2478 化学结构 CAS号:819812-04-9
KW-2478 3D分子结构 CAS号:819812-04-9
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KW-2478 纯度/质量文件 产品仅供科研

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KW-2478 生物活性

描述 KW-2478 functions as an Hsp90 inhibitor, displaying an IC50 of 3.8 nM against Hsp90α. It exhibits anti-proliferative effects on multiple myeloma (MM) and non-Hodgkin’s lymphoma (NHL), with GI50 values as follows: 0.30 μM (OPM-2/GFP), 0.34 μM (KMS-11), 0.39 μM (RPMI 8226), 0.12 μM (NCI-H929), 0.36 μM (Raji), 0.098 μM (SR), and 0.33 μM (SC-1). Moreover, KW-2478 impedes the transcription of c-Maf and Cyclin D1 genes primarily through the inhibition of Cdk9 activity [1].
体内研究

KW-2478, administered intravenously at doses ranging from 25 to 200 mg/kg, suppresses tumor growth in SCID mice implanted with NCI-H929 cells, without inducing weight loss. At a dose of 100 mg/kg, intravenously administered KW-2478 leads to the degradation of Hsp90 client proteins (IGF-1Rβ, c-Raf-1, Cdk9) and dephosphorylation of Erk1/2 proteins in NCI-H929 tumors in mice [1].

体外研究

KW-2478 functions as an Hsp90 inhibitor, displaying an IC50 of 3.8 nM against Hsp90α. It exhibits anti-proliferative effects on multiple myeloma (MM) and non-Hodgkin’s lymphoma (NHL), with GI50 values as follows: 0.30 μM (OPM-2/GFP), 0.34 μM (KMS-11), 0.39 μM (RPMI 8226), 0.12 μM (NCI-H929), 0.36 μM (Raji), 0.098 μM (SR), and 0.33 μM (SC-1). Moreover, KW-2478 impedes the transcription of c-Maf and Cyclin D1 genes primarily through the inhibition of Cdk9 activity [1].

KW-2478 参考文献

[1]Nakashima T, et al. New molecular and biological mechanism of antitumor activities of KW-2478, a novel nonansamycin heat shock protein 90 inhibitor, in multiple myeloma cells. Clin Cancer Res. 2010 May 15;16(10):2792-802.

KW-2478 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.74mL

0.35mL

0.17mL

8.70mL

1.74mL

0.87mL

17.40mL

3.48mL

1.74mL

KW-2478 技术信息

CAS号819812-04-9
分子式C30H42N2O9
分子量 574.663
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,Store in freezer, under -20°C

溶解方案

DMSO: 190 mg/mL(330.63 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

30% propylene glycol+5% Tween 80+65% water 10 mg/mL suspension

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