Amsilarotene (C09-1102-019)

Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α ( RAR-α ) binding with K i of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer , hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer .In VitroAmsilarotene (0, 10, 25 μM; 24 hours) induces apoptosis of human epithelial ovarian carcinoma-derived cell lines in a concentration-dependent manner. Amsilarotene (10, 20 μM; 0, 3, 6, and 9 days) inhibits the proliferation of BxPC-3 and MIAPaCa-2 cells. Amsilarotene (10 μM; 48 hours) increases the proportion of sensitive BxPC-3 cells in the G 1 phase. Amsilarotene (10 μM; 0, 3, 6, 24, 48, 72 hours) inhibits the retinoblastoma-gene product (RB) phosphorylation in BxPC-3 cells between 24 and 72 hours. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: RMG-I, RMG-II, RTSG, RMUG-S, RMUG-L, and KF cells Concentration: 0, 10, 25 μM Incubation Time: 24 hours Result: Induced apoptosis in a concentration-dependent manner in all of the cell lines, except KF cells. Cell Proliferation AssayCell Line: BxPC-3, MIAPaCa-2, AsPC-1 cells Concentration: 10 and 20 μM Incubation Time: 0, 3, 6, and 9 days. Result: Inhibited the proliferation of BxPC-3 and MIAPaCa-2 cells, but not the proliferation of AsPC-1 cells. Cell Cycle AnalysisCell Line: Sensitive BxPC-3 cells Concentration: 10 μM Incubation Time: 48 hours Result: The proportion of cells in the G 1 phase increased from 43% of untreated control cells to 86%In VivoAmsilarotene (8 mg/kg/day orally for 30 days) inhibits the RMG-II tumor growth in nude mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-week-old female BALB/c nu/nu mice with subcutaneous RMG-II tumorsDosage: 8 mg/kg/day Administration: Orally for 30 days Result: The maximal tumor growth-inhibiting effect was seen on day 31 of administration, when there was a 45% reduction of relative tumor volume (RTV).Form:Solid. Specification: 0.99 Molecular Formula: C20H27NO3Si2 Molecular Weight: 385.6 PubChem CID: 9800306 Isomeric SMILES: C[Si](C)(C)C1=CC(=CC(=C1)C(=O)NC2=CC=C(C=C2)C(=O)O)[Si](C)(C)C