AZD5153 is a potent bivalent triazolopyridazine based Bromodomain and Extraterminal (BET) Inhibitor, with IC50 value of 5 nM. AZD5153 could significantly disrupt BRD4 foci, with IC50 value of 1.7 nM in U2OS cells. AZD5153 could inhibit the proliferation of AML, MM, and DLBCL cell lines, with the majority of cell lines having a GI50 value < 25 nM. Furthermore, 200 nM AZD5153 could significantly decrease the level of mTOR pathway associated proteins in sensitive hematologic cancer cell lines (MOLP8, MV-4-11, OCILY19).
In AML, MM, and DLBCL xenografted tumor mouse models, oral administration of AZD5153 at the dose of 1, 2.5, and 5mg/kg could inhibit tumor growth in a dose dependent manner.
| Molecular Weight | 479.6 |
| Formula | C25H33N7O3 |
| CAS Number | 1869912-39-9 |
| Solubility (25°C) | DMSO ≥ 10 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.
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