CPI-1205 (Lirametostat) is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2. CPI-1205 has IC50 values of 2 nM and 52 nM for EZH2 and EZH1, respectively. CPI-1205 selectively inhibits the activity of both wild-type and mutated forms of EZH2, this specifically prevents the methylation of histone H3 on lysine 27 (H3K27). Decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased proliferation of EZH2-expressing cancer cells.
| Molecular Weight | 518.57 |
| Formula | C27H33F3N4O3 |
| CAS Number | 1621862-70-1 |
| Solubility (25°C) | DMSO ≥ 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related EZH2 Products |
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| Tulmimetostat
Tulmimetostat is an orally active dual EZH1/EZH2 protein inhibitor with antitumor activity for use in a variety of solid tumor studies. |
| PF-06821497
PF-06821497 is a selective and orally active Zeste Homolog 2 (EZH2) inhibitor with powerful tumor growth inhibition. |
| Valemetostat
Valemetostat (DS-3201, DS-3201b) is a first-in-class dual inhibitor targeting EZH1 and EZH2. It can be used in the study of adult T-cell leukemia/lymphoma. |
| MS1943
MS1943 is a pioneering oral bioactive selective EZH2 inhibitor with an IC50 of 120 nM. MS1943 significantly reduced EZH2 protein levels in many triple negative breast and other cancers and non-cancer lines. MS1943 effectively blocked the proliferation of multiple triple negative breast cancers and other cancer lines. |
| CPI-169 racemate
CPI-169 racemate is the racemate form of CPI-169, which is a novel and potent EZH2 inhibitor with IC50 <1 nM(inhibition of the catalytic activity of PRC2); decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis in a variety of cell lines. |
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