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

VER-50589 Chemical Structure

CAS No. : 747413-08-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1639
In-stock
1 mg ¥440
In-stock
5 mg ¥1490
In-stock
10 mg ¥2480
In-stock
50 mg ¥5860
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
DU-145 GI50
0.23 μM
Compound: 33
Growth inhibition of human DU145 cells by SRB assay
Growth inhibition of human DU145 cells by SRB assay
[PMID: 18020435]
HCT-116 GI50
0.12 μM
Compound: 33
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]
PC-3M GI50
0.22 μM
Compound: 33
Growth inhibition of human PC3M cells by SRB assay
Growth inhibition of human PC3M cells by SRB assay
[PMID: 18020435]
SF-268 GI50
0.034 μM
Compound: 33
Growth inhibition of human SF268 cells by SRB assay
Growth inhibition of human SF268 cells by SRB assay
[PMID: 18020435]
SK-MEL-28 GI50
0.045 μM
Compound: 33
Growth inhibition of human SKMel28 cells by SRB assay
Growth inhibition of human SKMel28 cells by SRB assay
[PMID: 18020435]
U-87MG ATCC GI50
0.028 μM
Compound: 33
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-50589 是一种 Hsp90 抑制剂,IC50 为 21 nM,Kd 为 4.5 nM。VER-50589 抑制全长重组酵母 Hsp90 的内在 ATPase,在 400 μM ATP 存在下,IC50 为 143 ± 23 nM。VER-50589 对多种人类癌细胞具有抗增殖活性,对于 CH1 人类卵巢细胞,最低 GI50 为 32.7 ± 0.2 nM,平均 GI50 为 78 ± 15纳米。VER-50589 抑制人脐静脉内皮细胞 (HUVEC) 的增殖,GI50 值为 19 ± 2.4 nM,对非致瘤性人乳腺显示出更高的 GI50s (MCF10a) 和前列腺 (PNT2) 上皮细胞。此外,VER-50589 显示同基因细胞系的细胞活性没有差异,并且这些活性与 NQO1 表达无关。VER-50589 还会导致 G1 和 G2-M 阻滞 (115 或 575 nM) 并在 HCT116 结肠癌细胞中诱导细胞生长抑制。此外,VER-50589 在 HCT116 细胞中引起大量摄取[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,ip) 在携带成熟的 OVCAR3 人卵巢腹水瘤的无胸腺小鼠中发挥完全的 HSP90 抑制作用。与对照组小鼠相比,VER-50589 (100 mg/kg,腹腔注射) 显示 HCT116 结肠癌异种移植物的肿瘤体积和肿瘤重量减少[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
细胞实验: 

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
目录号:
HY-15984
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