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| Cas No.: | 1621375-32-3 |
| Chemical Name: | VPC-14449 |
| Synonyms: | VPC-14449;4-(4-(2,4-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine;4-[4-(2,4-dibromoimidazol-1-yl)-1,3-thiazol-2-yl]morpholine |
| SMILES: | BrC1=NC(=C([H])N1C1=C([H])SC(=N1)N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H])Br |
| Formula: | C10H10Br2N4Os |
| M.Wt: | 394.0856 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | VPC 14449 is a potent and selective androgen receptor DNA-binding domain (AR-DBD) inhibitor with IC50 of 0.34 uM, without affecting AR protein expression; effectively blocks transcriptional activity of full-length and splice variant AR forms at low to sub-micromolar concentrations; reduces tumor volume and abolishes PSA production in LNCaP xenograft model. |
| In Vivo: | VPC-14449 (100 mg/kg; i.p. twice daily for 4 weeks) reduces tumor volume and abolishes PSA production with no decrease in body weight over a total duration 4 weeks in LNCaP xenograft model |
| In Vitro: | VPC-14449 (0.01-100 μM; 24 h) inhibits AR-transcriptional activity and cell viability in LNCaP, C4-2, MR49F, and 22Rv1 cells. VPC-14449 (0.01-100 μM; 24 h) dose-dependently inhibits the transiently expressed full-length human AR in PC3 cells |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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