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VER-82576 (NVP-BEP800) is a potent, orally available and selective inhibitor of Hsp90β with an IC50 of 58 nM. VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively. In A375 melanoma and BT-474 breast cancer cell lines, VER-82576 (NVP-BEP800) induced client protein degradation (including ErbB2, B-Raf(V600E), Raf-1, and Akt) and Hsp70 induction. Oral administration of NVP-BEP800 was well tolerated and induced robust antitumor responses in tumor xenograft models, including regression in the BT-474 breast cancer model. In these tumor models, NVP-BEP800 modulated Hsp90 client proteins and downstream signaling pathways at doses causing antitumor activity. NVP-BEP800 (VER-82576) can radiosensitise tumour cell lines of different entities through destabilisation and depletion of several Hsp90 client proteins, thus causing the depletion of S phase and G2/M arrest, increased DNA damage and repair protraction and, to some extent, apoptosis. VER-82576 (15 or 30 mg/kg, p.o.) shows antitumor activities in A375 cancer xenografts and BT-474 xenograft-bearing mice.
| Cell Experiment | |
|---|---|
| Cell lines | BT-474, SKBr3, MCF-7, MDA-MB-157, MDA-MB-231, MDA-MB-468 and BT20 cells line |
| Preparation method | Cell proliferation was determined using either sulforhodamine B for adherent cells or MTS assay for suspension cells or those showing low adherence. GI50 was the compound concentration that inhibits cell growth by 50% compared with vehicle control. |
| Concentrations | 0~1 μ M |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | T-474 tumor xenografts in nude mice |
| Formulation | 0.5% methyl cellulose |
| Dosages | 30 mg/kg qd for 2 weeks |
| Administration | PO. |
| Molecular Weight | 480.41 |
| Formula | C21H23Cl2N5O2S |
| CAS Number | 847559-80-2 |
| Solubility (25°C) | DMSO 5 mg/mL Ethanol 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HSP Products |
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BIIB021 (CNF2024) is an orally available synthetic non-ansamycin Hsp90 inhibitor with ki value of 1.7nM. |
| CUDC-305
CUDC-305 is a heat shock protein 90 (HSP90) inhibitor of the novel imidazopyridine class, with IC50 values of 100 and 103 nM for HSP90α and HSP90β, respectively. |
| Ganetespib
Ganetespib (STA-9090) is a potent synthetic small molecule inhibitor of Hsp90 with potential antineoplastic activity. |
| Luminespib (AUY922)
Luminespib (AUY922) is a small molecule Heat Shock Protein 90 (HSP90) inhibitor with IC50 values of 13 and 21 nM for HSP90α and HSP90β respectively. |
| NVP-HSP990
NVP-HSP990 is an orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively. NVP-HSP990 has potential antineoplastic activity. |
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