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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 | |
|---|---|
| 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 | |
|---|---|
| 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 |
| Related TAM Receptor Products |
|---|
| Bemcentinib
Bemcentinib (R428) is a potent and selective small-molecule inhibitor of Axl kinase with IC50 of 14 nM. |
| SGI-7079
SGI-7079 is a novel Axl inhibitor. |
| UNC2881
UNC2881 is a specific Mer tyrosine kinase inhibitor with IC50 of 4.3 nM, about 83- and 58-fold selectivity over Axl and Tyro3, respectively |
| Dubermatinib
Dubermatinib (TP-0903) is a potent and selective AXL inhibitor with an IC50 value of 27 nM. |
| RU-301
RU-301 is a pan-TAM receptor inhibitor that blocks Gas6-induced TAM activation and tumorigenicity, with Kd and IC50 values of 12 μM and 10 μM, respectively. |
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