1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  2. HSP Apoptosis
  3. VER-50589

VER-50589 是一种 Hsp90 抑制剂,IC50 值为 21 nM,Kd 值为 4.5 nM。

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VER-50589 Chemical Structure

VER-50589 Chemical Structure

CAS No. : 747413-08-7

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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 ¥1980
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1 mg ¥540
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5 mg ¥1800
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10 mg ¥3000
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50 mg ¥9500
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200 mg   询价  

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 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-50589 is a Hsp90 inhibitor, with an IC50 of 21 nM and a Kd of 4.5 nM.

IC50 & Target[1]

HSP90

21 nM (IC50)

体外研究
(In Vitro)

VER-50589 is a Hsp90 inhibitor, with an IC50 of 21 nM and a Kd of 4.5 nM. VER-50589 inhibits intrinsic ATPase of full-length recombinant yeast Hsp90, with an IC50 of 143 ± 23 nM in the presence of 400 μM ATP. VER-50589 shows antiproliferative activities against various human cancer cells, with the lowest GI50 of 32.7 ± 0.2 nM for CH1 human ovarian cells, and mean GI50 of 78 ± 15 nM. VER-50589 suppressses the proliferation of human umbilical vein endothelial cells (HUVEC) with GI50 value of 19 ± 2.4 nM, and shows higher GI50s against nontumorigenic human breast (MCF10a) and prostate (PNT2) epithelial cells. Furthermore, VER-50589 displays no differences in cellular activities of isogenic cell lines, and these activities are independent of NQO1 expression. VER-50589 also causes G1 and G2-M block (115 or 575 nM) and induces cytostasis in HCT116 colon cancer cells. In addition, VER-50589 causes great uptake in HCT116 cells[1].

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

体内研究
(In Vivo)

VER-50589 (4 mg/kg, i.p.) exerts a complete HSP90 inhibition in the athymic mice bearing well-established OVCAR3 human ovarian ascites tumors. VER-50589 (100 mg/kg, i.p.) shows reduced tumor volume and tumor weights in the HCT116 colon carcinoma xenografts compared to the control mice group[1].

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

分子量

388.80

Formula

C19H17ClN2O5

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
In Vitro: 

DMSO 中的溶解度 : ≥ 48 mg/mL (123.46 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5720 mL 12.8601 mL 25.7202 mL
5 mM 0.5144 mL 2.5720 mL 5.1440 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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Cell Assay
[1]

HCT116 and HT29 human colon cancer cells are seeded and left to attach overnight. Vehicle control or compound (VER-50589) is added for 1, 4, and 24 h. Attached cells are collected and counted by hemacytometer. Incubation medium (1 mL) and cell pellets are frozen at −80°C until mass spectrometry analysis[1].

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

Animal Administration
[1]

HCT116 cells (2-5 million cells per site) are injected s.c. in the flanks of 6- to 8-week-old female NCr athymic mice. Dosing commenced when tumors are well established (∼5-6 mm diameter). For combined therapy and pharmacokinetic and pharmacodynamic studies, mice bearing HCT116 xenografts are administered 100 mg/kg VER-50589 i.p. per day for 9 days. Tumor volumes are calculated. On study termination, blood samples are taken, and plasma is separated and stored −80°C. Tumors are excised, weighed, and snap frozen at −80°C[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 2.5720 mL 12.8601 mL 25.7202 mL 64.3004 mL
5 mM 0.5144 mL 2.5720 mL 5.1440 mL 12.8601 mL
10 mM 0.2572 mL 1.2860 mL 2.5720 mL 6.4300 mL
15 mM 0.1715 mL 0.8573 mL 1.7147 mL 4.2867 mL
20 mM 0.1286 mL 0.6430 mL 1.2860 mL 3.2150 mL
25 mM 0.1029 mL 0.5144 mL 1.0288 mL 2.5720 mL
30 mM 0.0857 mL 0.4287 mL 0.8573 mL 2.1433 mL
40 mM 0.0643 mL 0.3215 mL 0.6430 mL 1.6075 mL
50 mM 0.0514 mL 0.2572 mL 0.5144 mL 1.2860 mL
60 mM 0.0429 mL 0.2143 mL 0.4287 mL 1.0717 mL
80 mM 0.0322 mL 0.1608 mL 0.3215 mL 0.8038 mL
100 mM 0.0257 mL 0.1286 mL 0.2572 mL 0.6430 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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VER-50589
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HY-15984
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