| Name | UNC2025 |
| Description | UNC2025 (mrx-6313)(IC50 of 0.74 nM and 0.8 nM) is a potent and orally bioavailable dual MER/FLT3 inhibitor. UNC-2025 is about 20-fold selectivity higher than Axl and Tyro3. |
| In vitro | In 697 B-ALL cells, UNC-2025 potently inhibits Mer phosphorylation with IC50 of 2.7 nM. In A549 NSCLC and Molm-14 AML cell lines, UNC-2025 causes significant inhibition of colony formation dependent on Mer8 and Flt3. [1] In H2228 and H1299 cell lines, UNC-2025 inhibits MERTK oncogenic signaling downstream, such as basal and stimulated pAKT and pERK1/2. In four NSCLC cell lines, UNC-2025 also induces apoptotic cell death, and decreases colony formation. [2] |
| In vivo | In mice bearing 697 acute leukemia tumors, UNC-2025 (3 mg/kg, p.o.) shows good solubility and DMPK properties, and results in effective target inhibition. [1] In mice bearing H2228 or A549 tumors, UNC-2025 (50 mg/kg, p.o.) inhibits tumor growth. [2] |
| Storage | 02 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : Insoluble
Ethanol : 8 mg/mL (16.78 mM), Heating is recommended.
DMSO : 35.71 mg/mL (74.92 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (8.39 mM), Sonication is recommended.
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| Keywords | UNC2025 | Tyro3 | TAMReceptor | TAM Receptor | MERTK | Mer | leukemia | Inhibitor | inhibit | Fms like tyrosine kinase 3 | FLT3 | Cluster of differentiation antigen 135 | CD135 | cancer | AXL | acute |
| Inhibitors Related | Bemcentinib | Gilteritinib | Sunitinib | Fostamatinib | Nintedanib | Ripretinib | Sorafenib | Pexidartinib | Tepotinib | Brigatinib | Cabozantinib S-malate | Onatasertib |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Hematonosis Compound Library | Angiogenesis related Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | Anti-Cancer Active Compound Library |
United States
