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

VER-50589 是一種 Hsp90 抑制劑，IC50 值為 21 nM，Kd 值為 4.5 nM。

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VER-50589 Chemical Structure

VER-50589 Chemical Structure

CAS No. : 747413-08-7

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3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)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   詢價  
200 mg   詢價  

* Please select Quantity before adding items.

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻

查看 HSP 亞型特異性產(chǎn)品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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)

細胞效力
(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]
體外研究
(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.
體內(nèi)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 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : ≥ 48 mg/mL (123.46 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻
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.
參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱：
VER-50589
目錄號：
HY-15984
需求量：