CeMMEC13 is a potent inhibitor of the second bromodomain of the transcription initiation factor TAF1 with an an IC50 value of 2.1 μM and with minimal inhibition of BRD4, BRD9, CREBBP, or EP300. CeMMEC13 was found to synergize with BRD4 inhibitor (S)-JQ1 to arrest the proliferation of leukemia cell line THP1 and lung adenocarcinoma cell line H23.
| Molecular Weight | 336.34 |
| Formula | C19H16N2O4 |
| CAS Number | 1790895-25-8 |
| Form | Solid |
| Solubility (25°C) | DMSO: 5 mg/mL (warmed) |
| 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.
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