1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. HSP
  3. VER-49009

VER-49009  (Synonyms: CCT 129397)

目录号: HY-15986 纯度: 99.45%
Data Sheet SDS COA 产品使用指南

VER-49009 是一种 Hsp90 抑制剂,IC50 值为 25 nM,Kd 值为 78 nM。

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VER-49009 Chemical Structure

VER-49009 Chemical Structure

CAS No. : 558640-51-0

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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1664
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2 mg ¥990
In-stock
5 mg ¥1950
In-stock
10 mg ¥3300
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50 mg   询价  
100 mg   询价  

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM and a Kd of 78 nM.

IC50 & Target

HSP90

25 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
DU-145 GI50
1.2 μM
Compound: 6, VER-49009
Growth inhibition of human DU145 cells by SRB assay
Growth inhibition of human DU145 cells by SRB assay
[PMID: 18020435]
HCT-116 GI50
0.26 μM
Compound: 6, VER-49009
Growth inhibition of human HCT116 cells after 24 hrs by SRB assay
Growth inhibition of human HCT116 cells after 24 hrs by SRB assay
[PMID: 18020435]
NCI-H1975 GI50
1 μM
Compound: 2, VER-49009
Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells after 1 to 3 days by MTS assay
Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells after 1 to 3 days by MTS assay
[PMID: 24345447]
PC-3M GI50
2.2 μM
Compound: 6, VER-49009
Growth inhibition of human PC3M cells by SRB assay
Growth inhibition of human PC3M cells by SRB assay
[PMID: 18020435]
SF-268 GI50
0.32 μM
Compound: 6, VER-49009
Growth inhibition of human SF268 cells by SRB assay
Growth inhibition of human SF268 cells by SRB assay
[PMID: 18020435]
SK-BR-3 EC50
0.35 μM
Compound: 3, VER-49009
Inhibition of Hsp90alpha in human SKBR3 cells assessed as ErbB2 degradation by Western blot analysis
Inhibition of Hsp90alpha in human SKBR3 cells assessed as ErbB2 degradation by Western blot analysis
[PMID: 21106457]
SK-BR-3 EC50
0.5 μM
Compound: 3, VER-49009
Inhibition of Hsp90alpha in human SKBR3 cells assessed as up-regulation of HSP70 protein by Western blot analysis
Inhibition of Hsp90alpha in human SKBR3 cells assessed as up-regulation of HSP70 protein by Western blot analysis
[PMID: 21106457]
SK-MEL-28 GI50
0.48 μM
Compound: 6, VER-49009
Growth inhibition of human SKMel28 cells by SRB assay
Growth inhibition of human SKMel28 cells by SRB assay
[PMID: 18020435]
U-87MG ATCC GI50
1.2 μM
Compound: 6, VER-49009
Growth inhibition of human U87MG cells by SRB assay
Growth inhibition of human U87MG cells by SRB assay
[PMID: 18020435]
体外研究
(In Vitro)

VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM. VER-49009 binds to the ATPase of full length yeast Hsp90 protein, with an IC50 of 140 nM[1]. VER-49009 inhibits Hsp90, with a Kd of 78 nM. VER-49009 also shows antiproliferative activities against various human cancer cells, with a mean GI50 of 685 ± 119 nM. VER-49009 suppressses the proliferation of human umbilical vein endothelial cells (HUVEC) with GI50 values of 444 ± 91.1 nM, and shows higher GI50s against nontumorigenic human breast (MCF10a) and prostate (PNT2) epithelial cells. VER-49009 displays no differences in cellular activities of isogenic cell lines, and these activities are independent of NQO1 expression[2]. VER-49009 inhibits the proliferation (1, 2.5 μM), induces G2 phase arrest and reduces total Akt and phospho-Akt expression levels in CFSC cells (1-5 μM)[3].

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

体内研究
(In Vivo)

VER-49009 (4 mg/kg, i.p.) results in clear depletion of ERBB2 at 3 and 8 h following the final dose, with client protein levels returning to normal by 24 h, in the athymic mice bearing well-established OVCAR3 human ovarian ascites tumors[2].

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

分子量

387.82

Formula

C19H18ClN3O4

CAS 号
性状

固体

颜色

White to off-white

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
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (257.85 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 2.5785 mL 12.8926 mL 25.7852 mL
5 mM 0.5157 mL 2.5785 mL 5.1570 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

动物实验:

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: ≥ 2.75 mg/mL (7.09 mM); 澄清溶液

    此方案可获得 ≥ 2.75 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 27.5 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% Corn Oil

    Solubility: ≥ 2.75 mg/mL (7.09 mM); 澄清溶液

    此方案可获得 ≥ 2.75 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

扫码获得
动物溶解方案

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 PEG300/PEG400Tween 80,均可在 MCE 网站选购。
纯度 & 产品资料
参考文献
Cell Assay
[3]

Briefly, 5 × 103 cells/well are plated in 96-well culture plates. After an overnight incubation, the cells are treated with various concentrations of VER-49009 and VER-49009M (0, 1, 2.5, and 5 μM) for 24 h[3].

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

Animal Administration
[2]

In some studies, female NCr athymic mice are implanted i.p. with 10 million OVCAR3 ovarian carcinoma cells harvested from donor mice. This tumor mimics late-stage malignant disease. Once tumors are well established, mice are injected i.p. with 4 mg/kg VER-49009 or VER-50589 twice daily over 2 days (four doses total). Tumors are harvested at intervals after the last dose and snap frozen for pharmacodynamic analyses[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 2.5785 mL 12.8926 mL 25.7852 mL 64.4629 mL
5 mM 0.5157 mL 2.5785 mL 5.1570 mL 12.8926 mL
10 mM 0.2579 mL 1.2893 mL 2.5785 mL 6.4463 mL
15 mM 0.1719 mL 0.8595 mL 1.7190 mL 4.2975 mL
20 mM 0.1289 mL 0.6446 mL 1.2893 mL 3.2231 mL
25 mM 0.1031 mL 0.5157 mL 1.0314 mL 2.5785 mL
30 mM 0.0860 mL 0.4298 mL 0.8595 mL 2.1488 mL
40 mM 0.0645 mL 0.3223 mL 0.6446 mL 1.6116 mL
50 mM 0.0516 mL 0.2579 mL 0.5157 mL 1.2893 mL
60 mM 0.0430 mL 0.2149 mL 0.4298 mL 1.0744 mL
80 mM 0.0322 mL 0.1612 mL 0.3223 mL 0.8058 mL
100 mM 0.0258 mL 0.1289 mL 0.2579 mL 0.6446 mL

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产品名称:
VER-49009
目录号:
HY-15986
需求量:
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