1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. HSP
  3. KW-2478

KW-2478 是一种 Hsp90α 抑制剂,IC50 值为 3.8 nM,对多种人类血液肿瘤细胞具有抗肿瘤活性。

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KW-2478 Chemical Structure

KW-2478 Chemical Structure

CAS No. : 819812-04-9

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1896
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1 mg ¥650
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5 mg ¥1500
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10 mg ¥2400
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50 mg ¥5871
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100 mg ¥8224
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200 mg   询价  
500 mg   询价  

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.

IC50 & Target[1]

HSP90α

3.8 nM (IC50)

体外研究
(In Vitro)

KW-2478 is an inhibitor of Hsp90, with an IC50 of 3.8 nM for Hsp90α. KW-2478 shows anti-proliferative activity against multiple myeloma (MM) and non-Hodgkin’s lymphoma (NHL), with GI50s of 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 μM (SC-1). KW-2478 also inhibits the transcription of c-Maf and Cyclin D1 genes by mainly suppressing the function of Cdk9[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

KW-2478 (25-200 mg/kg, i.v.) inhibits tumor growth in combined immunodeficiency (SCID) mice bearing NCI-H929 cells, without body weight loss. KW-2478 (100 mg/kg, i.v.) causes degradation of the Hsp90 client proteins (IGF-1Rβ, c-Raf-1, Cdk9) levels and dephosphorylated Erk1/2 proteins in NCI-H929 tumors of mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

574.66

Formula

C30H42N2O9

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 200 mg/mL (348.03 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7402 mL 8.7008 mL 17.4016 mL
5 mM 0.3480 mL 1.7402 mL 3.4803 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (8.70 mM); 澄清溶液

    此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (8.70 mM); 澄清溶液

    此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.90%

参考文献
Cell Assay
[1]

The cells are plated into 96-well plates and treated with KW-2478. After 72 hours of cultivation, cell viability is determined using WST-1. WST reagent is added to the wells, followed by incubation for 4 hours at 37°C. After that, the absorbance at 450 nm with reference at 650 nm is measured with a microplate spectrophotometer[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Severe combined immunodeficient (SCID) mice are intraperitoneally injected with anti-asialo GM1 antibody. The next day, all mice are subcutaneously inoculated with NCI-H929 cells (1×107 cells) suspended in PBS containing 50% of Matrigel. After 10 days, tumor volume is measured using the Antitumor test system II, a computer-operated system including software and instruments. SCID mice with tumors (190 to 290 mm3) are selected. After randomly grouping, saline (vehicle) or KW-2478 is intravenously administered to mice once or twice daily for 5 days. 17-AAG is intravenously administered to mice. Tumor volume is calculated by the Anti-tumor test system II as follows: Tumor volume=DL×DS×DS×1/2. Fourteen days after the initial administration, blood samples of each mouse are obtained, followed by measurement of serum M protein (Ig kappa chain) with Human Kappa-b&f ELISA Quantitation Kit. The statistical analysis is performed using SAS software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7402 mL 8.7008 mL 17.4016 mL 43.5040 mL
5 mM 0.3480 mL 1.7402 mL 3.4803 mL 8.7008 mL
10 mM 0.1740 mL 0.8701 mL 1.7402 mL 4.3504 mL
15 mM 0.1160 mL 0.5801 mL 1.1601 mL 2.9003 mL
20 mM 0.0870 mL 0.4350 mL 0.8701 mL 2.1752 mL
25 mM 0.0696 mL 0.3480 mL 0.6961 mL 1.7402 mL
30 mM 0.0580 mL 0.2900 mL 0.5801 mL 1.4501 mL
40 mM 0.0435 mL 0.2175 mL 0.4350 mL 1.0876 mL
50 mM 0.0348 mL 0.1740 mL 0.3480 mL 0.8701 mL
60 mM 0.0290 mL 0.1450 mL 0.2900 mL 0.7251 mL
80 mM 0.0218 mL 0.1088 mL 0.2175 mL 0.5438 mL
100 mM 0.0174 mL 0.0870 mL 0.1740 mL 0.4350 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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目录号:
HY-13468
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