CPI-1205
- CAS No.
- 1621862-70-1
- Chemical Name:
- CPI-1205
- Synonyms
- 1205;CPDB1215;CPI-1205;CPI‑CPI-1205 (CPI 1205;Lirametostat ( CPI-1205 );N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-1-[(1R)-1-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]ethyl]indole-3-carboxamide;(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;1H-Indole-3-carboxamide, N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-[1-(2,2,2-trifluoroethyl)-4-piperidinyl]ethyl]-
- CBNumber:
- CB33145567
- Molecular Formula:
- C27H33F3N4O3
- Molecular Weight:
- 518.57
- MDL Number:
- MOL File:
- 1621862-70-1.mol
| Boiling point | 692.5±55.0 °C(Predicted) |
|---|---|
| Density | 1.31±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | Soluble in DMSO |
| pka | 11.01±0.10(Predicted) |
| FDA UNII | 455J2479FY |
CPI-1205 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ApexBio Technology | B7819 | CPI-1205 | 1621862-70-1 | 50mg | $1733 | 2021-12-16 | Buy |
| Chemenu | CM328325 | N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-1-[(1R)-1-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]ethyl]indole-3-carboxamide 95%+ | 1621862-70-1 | 1g | $9280 | 2021-12-16 | Buy |
CPI-1205 Chemical Properties,Uses,Production
Biological Activity
0.002 μm for biochemical ic50; 0.032 μm for cellular ec50.cpi-1205 is an ezh2 inhibitor.polycomb repressive complex 2 (prc2) plays a key role in transcriptional silencing partially by installing methylation marks on lysine 27 of histone 3. dysregulation of prc2 function relates with certain malignancies and poor prognosis. ezh2 is thus representing a promising candidate oncology target for pharmacological intervention.
in vitro
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 [1].
in vivo
in animal study, cpi-1205 was dosed at 160 mg/kg orally twice daily for 25 days in tumor bearing female cb-17 scid mice. by the treatment of tumor-bearing mice with cpi-1205, tumor regression was observed within two weeks. by the end of day 25, significant tumor growth inhibition was recorded. cpi-1205 was found to be well-tolerated for repeat dosing as observed by the absence of significant body weight loss. in addition, analysis of plasma and tumor at 1 h post last dose on day 25 showed sufficient plasma and tumor tissue concentrations [1].
References
[1] vaswani rg et al. identification of (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 (cpi-1205), a potent and selective inhibitor of histone methyltransferase ezh2, suitable for phase i
CPI-1205 Preparation Products And Raw materials
Raw materials
Preparation Products
CPI-1205 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43348 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |
| WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd. | 17702719238 17702719238 | sales@sun-shinechem.com | China | 905 | 64 |
| MedChemexpress LLC | 021-58955995 | sales@medchemexpress.cn | United States | 4863 | 58 |