LIRAMETOSTAT

Name	CPI-1205
Synonyms	CPDB1215 CPI-1205 LIRAMETOSTAT 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]-
CAS	1621862-70-1

Molecular Formula	C27H33F3N4O3
Molar Mass	518.57
Density	1.31±0.1 g/cm3(Predicted)
Boling Point	692.5±55.0 °C(Predicted)
Solubility	DMSO
pKa	11.01±0.10(Predicted)
Storage Condition	-20℃
In vitro study	Treatment with EZH2 inhibitor CPI-1205 can lead to apoptosis in multiple myeloma and plasmacytoma cell models.
In vivo study	In in vivo experiments, CPI-1205 has excellent oral bioavailability. The animals tolerated CPI-1205 well over the course of repeated dosing without significant weight loss. In rats and dogs, CPI-1205 had relatively high blood clearance (Rat -3.19 L/h/kg, dog -1.41 L/h/kg). In both species, there is a relatively good oral availability, 44.6% and 46.2% respectively. In the toxicity test, it is well tolerated, during the recovery period, the toxic effect is reversible.

Last Update：2024-01-02 23:10:35

biological activity	Lirametostat (CPI-1205) is an inhibitor of selective histone lysine methyltransferase EZH2 with oral biological activity. The IC50 for EZH2 and EZH1 is 2 nM and 52 nM respectively. It has potential anti-tumor activity.
target	TargetValue EZH2 (Cell-Free Assay) 2 nM EZH1 (Cell-Free Assay) 52 nM
Target	Value
EZH2 (Cell-free assay)	2 nM
EZH1 (Cell-free assay)	52 nM
in vitro study	in multiple myeloma and plasmacytoma cell models, the treatment of EZH2 inhibitor CPI-1205 can lead to apoptosis.
in vivo research	in vivo experiments, CPI-1205 have excellent oral bioavailability. In the course of repeated administration, the animals had good tolerance to CPI-1205 without significant weight loss. In rats and dogs, CPI-1205 have relatively high blood clearance rates (rats -3.19 L/h/kg, dogs -1.41 L/h/kg). In these two species, there are relatively good oral utilization, 44.6% and 46.2% respectively. In the toxicity test, it is well tolerated, and during the recovery period, the toxic effect is reversible.

Last Update：2024-04-09 15:16:35

Product Name: CPI-1205 Visit Supplier Webpage Request for quotation
CAS: 1621862-70-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

Product Name: CPI-1205 Visit Supplier Webpage Request for quotation
CAS: 1621862-70-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

View History

LIRAMETOSTAT

LIRAMETOSTAT Request for Quotation