| CAS NO: | 558640-51-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 387.82 |
|---|---|
| Formula | C19H18ClN3O4 |
| CAS No. | 558640-51-0; |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 77 mg/mL (198.5 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| SMILES Code | O=C(C1=C(C2=CC=C(OC)C=C2)C(C3=CC(Cl)=C(O)C=C3O)=NN1)NCC |
| Synonyms | CCT0129397; CCT-0129397; CCT 0129397; VER 49009; VER49009; VER-49009. |
| In Vitro | In vitro activity: VER-49009 inhibits the intrinsic ATPase activity of recombinant yeast Hsp90 with IC50 of 167 nM, and produces antiproliferative activity in a panel of human cancer cell lines and nontumorigenic cells in vitro. VER-49009 causes induction of HSP72 and HSP27 with depletion of client proteins, including C-RAF, B-RAF, and survivin, and PRMT5, which further result in cell cycle arrest and apoptosis. VER-49009 inhibits the cell proliferation, and induces G2 phase arrest in hepatic stellate cell line CFSC cells, which may suggest a rational approach in the prevention of liver fibrosis. Kinase Assay: Binding of HSP90 inhibitors to human full-length recombinant HSP90β is determined by a competitive binding fluorescence polarization assay, using a fluorescent pyrazole resorcinol probe. Cell Assay: Antiproliferative effects are measured using the sulforhodamine B assay. HUVEC sensitivity is determined by an alkaline phosphatase method. Cells: Melanoma cells (SKMEL 2, SKMEL 5, SKMEL 28, WM266.4); Colon cancer cells (HCT116, BEneg, BE2, HT29, HT29oxaliR); Ovarian cancer cells (CH1, CH1doxR); Breast cancer cells (MB-231, MB-468, BT20, ZR751, MCF7, BT-474); nontumorigenic cells (HUVEC, MCF10a, PNT) |
|---|---|
| In Vivo | In athymic mice, VER-49009 (20 mg/kg, i.v.) shows rapid clearance with values of 0.187 L/h. In an orthotopic human ovarian carcinoma model, VER-49009 (4 mg/kg, i.p.) also induces the depletion of the sensitive HSP90 client protein ERBB2. |
| Animal model | Mice bearing established OVCAR3 human ovarian xenografts. |
| Formulation & Dosage | Dissolved in 10% DMSO, 5% Tween 20, 85% saline; 4 mg/kg; i.p. injection |
| References | Mol Cancer Ther. 2007 Apr;6(4):1198-211; Mol Cell Biochem. 2009 Oct;330(1-2):181-5. |
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