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| 2mg |
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Purity: ≥98%
VER-49009 (CCT0129397; VER 49009; CCT-0129397; VER49009), a pyrazole-based compound, is a novel, potent and selective inhibitor of HSP90 (Heat Shock Protein 90) with potential antitumor activity. It inhibits HSP90β with an IC50 of 47 nM. It shows high in vivo antitumor efficacy in ice bearing established OVCAR3 human ovarian xenografts.
| ln Vitro |
The Hsp90 inhibitor VER-49009 has an IC50 of 25 nM. With an IC50 of 140 nM, VER-49009 binds to the ATPase of the whole yeast Hsp90 protein[1]. Hsp90 is inhibited by VER-49009 at a Kd of 78 nM. With a mean GI50 of 685 ± 119 nM, VER-49009 also exhibits antiproliferative effects against different human cancer cells. With GI50 values of 444 ± 91.1 nM, VER-49009 inhibits the growth of human umbilical vein endothelial cells (HUVEC) and exhibits greater GI50s against nontumorigenic human breast (MCF10a) and prostate (PNT2) epithelial cells. The cellular activities of isogenic cell lines are not different in VER-49009, and these activities are not reliant on NQO1 expression[2]. In CFSC cells, VER-49009 suppresses proliferation (1, 2.5 μM), causes G2 phase arrest, and lowers total and phospho-Akt expression levels (1–5 μM)[3].
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| ln Vivo |
In athymic mice exhibiting well-established OVCAR3 human ovarian ascites tumors, VER-49009 (4 mg/kg, ip) causes a noticeable depletion of ERBB2 at 3 and 8 hours after the final dose, with client protein levels reverting to normal by 24 hours[2].
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| References |
[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.
[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. [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 |
| Molecular Formula |
C19H18CLN3O4
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| Molecular Weight |
387.82
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| CAS # |
558640-51-0
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| Related CAS # |
940289-57-6
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| SMILES |
O=C(C1=C(C2=CC=C(OC)C=C2)C(C3=CC(Cl)=C(O)C=C3O)=NN1)NCC
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (7.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (7.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2579 mL | 1.2893 mL | 2.5785 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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