CPI-169, a representative compound from that effort, inhibits the catalytic activity of PRC2 with an IC50 of < 1nM, decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis in a variety of cell lines. Importantly, compound treatment triggers a sequence of downstream functional consequences of EZH2 inhibition whereby apoptosis is not induced before ten days of continuous target engagement.
| Molecular Weight | 528.66 |
| Formula | C27H36N4O5S |
| CAS Number | 1450655-76-1 |
| 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 |
|---|
| 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. |
| CPI-1205
CPI-1205 is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2. |
| 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. |
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