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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 |
|---|
| UNC1062
UNC1062 is a MERTK-selective tyrosine kinase inhibitor, reduces activation of MERTK-mediated downstream signaling, induces apoptosis in culture, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. |
| AZ14145845
AZ14145845 is a highly selective type I1/2 dual Mer/Axl kinase inhibitor with in vivo efficacy. |
| Axl/Mer/CSF1R-IN-2
Axl/Mer/CSF1R-IN-2 is a Axl, Mer and CSF1R inhibitor. |
| AXL-IN-15
AXL-IN-15 is a potent Axl inhibitor with both Ki and IC50 <1 nM. |
| Glesatinib
Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC). |
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