VER-49009
Based on 1 Customer Validation
VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM and a Kd of 78 nM.
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- Pureté: 99.45%
- CAS No.: 558640-51-0
- Formule: C19H18ClN3O4
- Masse moléculaire:387.82
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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HSP90 25 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | GI50 |
1.2 μM
Compound: 6, VER-49009
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Growth inhibition of human DU145 cells by SRB assay
Growth inhibition of human DU145 cells by SRB assay
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[PMID: 18020435] |
| HCT-116 | GI50 |
0.26 μM
Compound: 6, VER-49009
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Growth inhibition of human HCT116 cells after 24 hrs by SRB assay
Growth inhibition of human HCT116 cells after 24 hrs by SRB assay
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[PMID: 18020435] |
| HCT-116 | GI50 |
0.26 μM
Compound: 11
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Inhibitory concentration against cell proliferation of human HCT116 cells
Inhibitory concentration against cell proliferation of human HCT116 cells
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[PMID: 15974572] |
| NCI-H1975 | GI50 |
1 μM
Compound: 2, VER-49009
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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
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[PMID: 24345447] |
| PC-3M | GI50 |
2.2 μM
Compound: 6, VER-49009
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Growth inhibition of human PC3M cells by SRB assay
Growth inhibition of human PC3M cells by SRB assay
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[PMID: 18020435] |
| SF-268 | GI50 |
0.32 μM
Compound: 6, VER-49009
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Growth inhibition of human SF268 cells by SRB assay
Growth inhibition of human SF268 cells by SRB assay
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[PMID: 18020435] |
| SK-BR-3 | EC50 |
0.25 μM
Compound: 3, VER-49009
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Cytotoxicity against human SKBR3 cells
Cytotoxicity against human SKBR3 cells
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[PMID: 21106457] |
| SK-BR-3 | EC50 |
0.35 μM
Compound: 3, VER-49009
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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
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[PMID: 21106457] |
| SK-BR-3 | EC50 |
0.5 μM
Compound: 3, VER-49009
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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
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[PMID: 21106457] |
| SK-MEL-28 | GI50 |
0.48 μM
Compound: 6, VER-49009
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Growth inhibition of human SKMel28 cells by SRB assay
Growth inhibition of human SKMel28 cells by SRB assay
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[PMID: 18020435] |
| U-87MG ATCC | GI50 |
1.2 μM
Compound: 6, VER-49009
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Growth inhibition of human U87MG cells by SRB assay
Growth inhibition of human U87MG cells by SRB assay
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[PMID: 18020435] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 558640-51-0
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Appearance Solid
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Masse moléculaire 387.82
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Formule C19H18ClN3O4
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Color White to off-white
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SMILES
O=C(C1=NNC(C2=CC(Cl)=C(O)C=C2O)=C1C3=CC=C(OC)C=C3)NCC
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Synonyms
CCT 129397
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
DMSO : 100 mg/mL (257.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (7.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Dymock BW, et al. Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design. J Med Chem. 2005 Jun 30;48(13):4212-5. [Content Brief]
[2]. Sharp SY, et al. Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues. Mol Cancer Ther. 2007 Apr;6(4):1198-211. [Content Brief]
[3]. Sun X, et al. Inhibition of hepatic stellate cell proliferation by heat shock protein 90 inhibitors in vitro. Mol Cell Biochem. 2009 Oct;330(1-2):181-5. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 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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