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Purity: ≥98%
NVP-BEP800 (VER-82576; NVP BEP-800; BEP-800) is a novel, potent, fully synthetic, orally bioavailable heat shock protein 90β (HSP90β) inhibitor with potential antitumor activity. It inhibits HSP90β with an IC50 of 58 nM. NVP-BEP800 exhibits excellent antitumor efficacy in the A375 melanoma xenograft model.
| ln Vitro |
Potent and selective Hsp90 inhibitor VER-82576 (NVP-BEP800) has an IC50 of 58 nM for Hsp90β and an IC50 of 4.1 ± 1.1 and 5.5 ± 0.48 μM for Grp94 and Trap-1, respectively, indicating >70-fold selectivity. With an average GI50 of 245 nM and GI50s ranging from 38 nM in A375 cells to 1050 nM in PC3 cells, VER-82576 potently suppresses the growth of tumor cells. Client proteins are depleted in human cancer cell lines in vitro by VER-82576 (250–1250 nM)[1]. VER-82576 (NVP-BEP800; 200 nM) is less hazardous to SNB19 cells and exhibits no discernible influence on the ionizing radiation (IR) dose-response curves of A549 cells. In both A549 and SNB19 cell lines, VER-82576 combined with IR causes more severe DNA damage than either treatment alone. It also delays the kinetics of DNA damage repair in SNB19 cells[2]. VER-82576 (NVP-BEP800; 0.05, 0.1, or 0.2 μM) reduces glioblastoma cell viability and causes apoptosis in a dose-dependent manner. In T98G cells, VER-82576 (0.2 μM) inhibits IKKβ protein expression but does not change IKKβ mRNA levels. Heat shock protein 70 expression is suppressed by VER-82576 at a concentration of 0.2 μM.
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| ln Vivo |
In A375 cancer xenografts and BT-474 xenograft-bearing mice, VER-82576 (NVP-BEP800; 15 or 30 mg/kg, po) exhibits anticancer activities[1].
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| References |
[1]. Massey AJ, et al. Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800. Mol Cancer Ther. 2010 Apr;9(4):906-19.
[2]. Niewidok N, et al. Hsp90 Inhibitors NVP-AUY922 and NVP-BEP800 May Exert a Significant Radiosensitization on Tumor Cells along with a Cell Type-Specific Cytotoxicity. Transl Oncol. 2012 Oct;5(5):356-69. Epub 2012 Oct 1. [3]. Wu J, et al. Irradiation facilitates the inhibitory effect of the heat shock protein 90 inhibitor NVP-BEP800 on the proliferation of malignant glioblastoma cells through attenuation of the upregulation of heat shock protein 70. Exp Ther Med. 2014 Sep;8(3) |
| Molecular Formula |
C21H23CL2N5O2S
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| Molecular Weight |
480.41
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| CAS # |
847559-80-2
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| SMILES |
O=C(C1=CC2=C(N=C(N=C2S1)N)C3=CC(OCCN4CCCC4)=C(C=C3Cl)Cl)NCC
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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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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0816 mL | 10.4078 mL | 20.8156 mL | |
| 5 mM | 0.4163 mL | 2.0816 mL | 4.1631 mL | |
| 10 mM | 0.2082 mL | 1.0408 mL | 2.0816 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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