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ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
| Molecular Weight | 562.48 |
| CAS Number | 761436-81-1 |
| Solubility (25°C) | DMSO ≥ 90 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 ALK Products |
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| Con B-1
ConB-1 is a strongly selective ALK inhibitor with low toxicity to normal cells. |
| WAY-270947
WAY-270947 is a ALK5 inhibitor. |
| Ensartinib dihydrochloride
Ensartinib dihydrochloride (X-396 dihydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. |
| MS4078
MS4078 is a PROTAC degrader of ALK which potently decreases cellular levels of oncogenic active ALK fusion proteins in SU-DHL-1 lymphoma and NCI-H2228 lung cancer cells. |
| Repotrectinib (TPX-0005)
Repotrectinib (TPX-0005) is a potential best-in-class ALK/ROS1/TRK inhibitor against SRC, wild-type WT ALK, The IC50 values of ALK G1202R and ALK L1196M were 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM, respectively. |
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