TNIK-IN-3 is a potent, selective and orally active TNIK inhibitor with an IC50 value of 0.026 μM. In addition, TNIK-IN-3 inhibits Flt4 (IC50=0.030 μM), Flt1 (IC50=0.191 μM) and DRAK1 (IC50=0.411 μM). -3 can be used in studies related to colorectal cancer.
| Molecular Weight | 387.41 |
| Formula | C23H18FN3O2 |
| CAS Number | 2754265-25-1 |
| Form | Solid |
| Solubility (25°C) | DMSO 83.33 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 TNIK Products |
|---|
| PF-794
PF-794 (PF-06279794) is a potent, selective, ATP-competitive TNIK inhibitor. |
| Jatrorrhizine
Jatrorrhizine, an isoquinoline alkaloid found in common medicinal plants, is also a TNIK inhibitor with antibacterial, anti-inflammatory and antitumor activities. |
| Mebendazole
Mebendazole is a highly effective, broad-spectrum antihelmintic indicated for the treatment of nematode infestations; has been found as a hedgehog inhibitor. |
| NCB-0846
NCB-0846 is a novel, orally small-molecule Wnt inhibitor that inhibits TNIK (TRAF2 and NCK-Interacting Kinase) with an IC50 value of 21 nM. |
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