Enbezotinib, an inhibitor of RET, can inhibit the RET autophosphorylation. Enbezotinib can be used for the research of cancer.
| Molecular Weight | 424.43 |
| Formula | C21H21FN6O3 |
| CAS Number | 2359649-81-1 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL (ultrasonic and warming and heat to 60°C) |
| 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 RET Products |
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| RET V804M-IN-1
RET V804M-IN-1 is a wt-RET -selective inhibitors of RETV804M kinase, with an IC50 of 20 nM. |
| Multi-kinase-IN-5
Multi-kinase-IN-5 is a promising multi-kinase inhibitory agent. |
| NSC194598
NSC194598 is a p53 DNA-binding inhibitor with IC50 value of 180 nM and 2-40 μM for in vitro and in vivo, respectively. |
| RET-IN-22
RET-IN-22 is a potent, selective and orally active RET inhibitor with an IC50 of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. |
| RET-IN-23
RET-IN-23 is a potent and orally active RET inhibitor with IC50 values of 1.32, 2.50, 6.54, 1.03, 1.47 nM for RET-WT, RET-CCDC6, RET-V804L, RET-V804M, RET-M918T, respectively. |
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