PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.
| Molecular Weight | 525.08 |
| Formula | C29H37ClN4O3 |
| CAS Number | 2070014-93-4 |
| Solubility (25°C) | DMSO 100 mg/mL Water 100 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.
[1] Viral N Shah, et al. Diabetes Technol Ther. Standardized Hybrid Closed-Loop System Reporting
[2] Jrme Paillassa, et al. Curr Treat Options Oncol. Biology and Treatment of Hairy Cell Leukemia
[3] Phyu Thin Naing, et al. Hairy Cell Leukemia
[4] Enrico Tiacci, et al. J Clin Oncol. Genomics of Hairy Cell Leukemia
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