WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206532
CAS#: 1621862-70-1
Description: Lirametostat, also known as CPI-1205 is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2. Upon oral administration, CPI-1205 selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 on lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased proliferation of EZH2-expressing cancer cells.
MedKoo Cat#: 206532
Name: Lirametostat
CAS#: 1621862-70-1
Chemical Formula: C27H33F3N4O3
Exact Mass: 518.2505
Molecular Weight: 518.5812
Elemental Analysis: C, 62.54; H, 6.41; F, 10.99; N, 10.80; O, 9.26
Synonym: CPI-1205; CPI 1205; CPI1205; Lirametostat;
IUPAC/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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 518.5812 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Vaswani RG, Gehling VS, Dakin LA, Cook A, Nasveschuk CG, Duplessis M, Iyer P,
Balasubramanian S, Zhao F, Good AC, Campbell R, Lee C, Cantone N, Cummings RT,
Normant E, Bellon SF, Albrecht BK, Harmange JP, Trojer P, Audia JE, Zhang Y,
Justin N, Chen S, Wilson J, Gamblin S. 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 Clinical Trials for B-Cell Lymphomas. J Med Chem. 2016 Oct 14. PubMed
PMID: 27739677.
