UNC2250 is a potent and selective Mer inhibitor with IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.
Cell Experiment | |
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Cell lines | BT-12 rhabdoid tumor cells, and Colo699 NSCLC cells |
Preparation method | Culturing BT-12 rhabdoid tumor cells (10 000 cells) in 2.0 mL of 0.35% soft agar containing 0.5× RPMI medium, 7.5% FBS, and the indicated concentrations of 10 or DMSO vehicle only and overlaid with 0.5 mL of 1× RPMI medium containing 15% FBS and 10 or DMSO vehicle only. Refreshing medium and 10 or vehicle twice a week. Staining colonies with thiazolyl blue tetrazolium bromide and counting after 3 weeks. Colo699 NSCLC cells (15 000 cells) are cultured in 1.5 mL of 0.35% soft agar containing 1× RPMI medium and 10% FBS and overlaid with 2.0 mL of 1× RPMI medium containing 10% FBS and the indicated concentrations of 10 or DMSO vehicle only. Refreshing medium and 10 or vehicle 3 times per week.Staining colonies with nitrotetrazolium blue chloride and counting after 2 weeks. |
Concentrations | ~3 μM for BT-12, ~300 nM for Colo699 |
Incubation time | 3 weeks for BT-12, 2 weeks for Colo699 |
Animal Experiment | |
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Animal models | Mice |
Formulation | |
Dosages | ~3 mg/kg |
Administration | i.v. or p.o. |
Molecular Weight | 440.58 |
Formula | C24H36N6O2 |
CAS Number | 1493694-70-4 |
Form | Solid |
Solubility (25°C) | DMSO |
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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