| CAS NO: | 747413-08-7 |
| 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) | 388.80 |
|---|---|
| Formula | C19H17ClN2O5 |
| CAS No. | 747413-08-7 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 77 mg/mL (198.0 mM) |
| Water: <1 mg/mL | |
| Ethanol: 77 mg/mL (198.0 mM) | |
| Other info | Chemical Name: 5-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)isoxazole-3-carboxamide InChi Key: JXPCDMPJCKNLBY-UHFFFAOYSA-N InChi Code: InChI=1S/C19H17ClN2O5/c1-3-21-19(25)17-16(10-4-6-11(26-2)7-5-10)18(27-22-17)12-8-13(20)15(24)9-14(12)23/h4-9,23-24H,3H2,1-2H3,(H,21,25) SMILES Code: O=C(C1=NOC(C2=CC(Cl)=C(O)C=C2O)=C1C3=CC=C(OC)C=C3)NCC |
| Synonyms | VER 50589; VER-50589; VER50589; |
| In Vitro | In vitro activity: VER-50589 inhibits the intrinsic ATPase activity of recombinant yeast Hsp90 with IC50 of 143 nM, and produces antiproliferative activity in a panel of human cancer cell lines and nontumorigenic cells in vitro. VER-50589 causes induction of HSP72 and HSP27 alongside depletion of client proteins, including C-RAF, B-RAF, and survivin, and the protein arginine methyltransferase PRMT5, which further result in cell cycle arrest and apoptosis. 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 HCT116 human colon cancer xenografts, VER-50589 (100 mg/kg i.p.) results in a statistically significant reduction of ~30% in tumor volume and weight, as well as induction of HSP72 and depletion of ERBB2 and C-RAF. |
| Animal model | HCT116 human colon cancer xenografts |
| Formulation & Dosage | Dissolved in 10% DMSO, 5% Tween 20, 85% saline; 100 mg/kg; i.p. injection |
| References | Mol Cancer Ther. 2007 Apr;6(4):1198-211. |
m.cnreagent.com