| CAS NO: | 1621862-70-1 |
| 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 |
| Molecular Weight (MW) | 518.57 |
|---|---|
| Formula | C27H33F3N4O3 |
| CAS No. | 1621862-70-1 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 100 mg/mL (192.8 mM) |
| Water: <1 mg/mL | |
| Ethanol: 100 mg/mL (192.8 mM) | |
| Other info | Chemical Name: (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide InChi Key: HPODOLXTMDHLLC-QGZVFWFLSA-N InChi Code: InChI=1S/C27H33F3N4O3/c1-16-13-23(37-4)21(25(35)32-16)14-31-26(36)24-18(3)34(22-8-6-5-7-20(22)24)17(2)19-9-11-33(12-10-19)15-27(28,29)30/h5-8,13,17,19H,9-12,14-15H2,1-4H3,(H,31,36)(H,32,35)/t17-/m1/s1 SMILES Code: C[C@@H](N1C2=C(C(C(NCC3=C(C=C(NC3=O)C)OC)=O)=C1C)C=CC=C2)C4CCN(CC(F)(F)F)CC4 |
| Synonyms | CPI1205; Lirametostat; CPI-1205; CPI 1205 |
| In Vitro | In vitro activity: Treatment with EZH2 inhibitor CPI-1205 cause apoptosis in multiple myeloma and plasmacytoma cell models Cell Assay: Previous study reported that the treatment with CPI-1205 caused apoptosis in multiple myeloma and plasmacytoma cell models. CPI-1205 also had a clean selectivity profile when tested against 30 other histone or DNA methyltransferases. In addition, CPI-1205 demonstrated modest selectivity when tested against enhancer of zeste homologue 1 (EZH1) that is a methyltransferase highly related to EZH2. |
|---|---|
| In Vivo | CPI-1205 shows excellent oral bioavailability. It was well-tolerated for repeat dosing as demonstrated by the absence of significant body weight loss. CPI-1205 shows relatively high clearance in both rats and dogs (3.19 L/h/kg and 1.41 L/h/kg, respectively) but demonstrates good oral bioavailability in both species(44.6% F in rats and 46.2% F in dogs). CPI-1205 was well-tolerated in the 28-day GLP toxicology studies, and any findings were reversible over the recovery period |
| Animal model | CB-17 SCID mice |
| Formulation & Dosage | Formulated in 10% DMSO + 60% PEG400 + 30% ddH2O; 160 mg/kg orally twice daily; oral gavage |
| References | J Med Chem. 2016 Nov 10;59(21):9928-9941. |
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