| Name | UNC2250 |
| Description | UNC2250 is an effective and specific Mer inhibitor (IC50=1.7 nM). |
| Cell Research | BT-12 rhabdoid tumor cells (10?000 cells) are cultured 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. Medium and 10 or vehicle are refreshed 2 times per week. Colonies were stained with thiazolyl blue tetrazolium bromide and counted 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. Medium and 10 or vehicle are refreshed 3 times per week. Colonies are stained with nitrotetrazolium blue chloride and counted after 2 weeks.(Only for Reference) |
| Kinase Assay | Microfluidic Capillary Electrophoresis (MCE) Assay: Activity assays are performed in a 384-well, polypropylene microplate in a final volume of 50 μL of 50 mM Hepes, pH 7.4, containing 10 mM MgCl2, 1.0 mM DTT, 0.01% Triton X-100, 0.1% bovine serum albumin (BSA), containing 1.0 μM fluorescent substrate and ATP at the Km for each enzyme. All reactions are terminated by addition of 20 μL of 70 mM EDTA. After an 180 min incubation, phosphorylated and unphosphorylated substrate peptides are separated in buffer supplemented with 1× CR-8 on a LabChip EZ Reader equipped with a 12-sipper chip. Data are analyzed using EZ Reader software. |
| In vivo | According to in vivo PK experiment, UNC2250 has a moderate half-life, clearance, and volume of distribution as well as reasonable oral bioavailability and good solubility. [1] |
| Storage | Store under nitrogen | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 20% Cremophor EL : 5 mg/mL (11.35 mM), Suspension.
DMSO : 25 mg/mL (56.74 mM), Sonication is recommended.
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| Keywords | UNC-2250 | UNC2250 | UNC 2250 | Tyro3 | TAMReceptor | TAM Receptor | Mer | Inhibitor | inhibit | Axl |
| Inhibitors Related | UNC2025 | Cabozantinib | Bemcentinib | Gilteritinib | UNC 1025 | Dubermatinib | Sitravatinib | NCT-503 | Tepotinib | Cabozantinib S-malate | AXL-IN-13 | BMS 777607 |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Multi-Target Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max |
United States
