CPI-1612 is a tool compound that appears to be a fairly efficient EP300/CBP histone acetyltransferase (HAT) inhibitor, exhibiting activity in xenograft models with good PK of higher species.
| Molecular Weight | 450.53 |
| Formula | C27H26N6O |
| CAS Number | 2374971-81-8 |
| Solubility (25°C) | DMSO ≥ 60 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 Histone Acetyltransferase Products |
|---|
| KAT modulator-1
KAT modulator-1 is a KAT modulator. |
| KAT6-IN-1
KAT6-IN-1 is a potent KAT6 inhibitor. |
| MC4171
MC4171 is a selective KAT8 inhibitor (IC50=8.1 µM). |
| MOZ-IN-3
MOZ-IN-3 is a KAT6A (MOZ) acetyltransferase inhibitor (IC50: 30 nM). |
| Ep300/CREBBP-IN-4
Ep300/CREBBP-IN-4 is a potent Ep300 and CREBBP inhibitor with IC50s of 0.024 and 0.064 μM, respectively. |
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