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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | H2O : Insoluble Ethanol : 8 mg/mL (15.59 mM), Heating is recommended. DMSO : 6.25 mg/mL (13.11 mM), Sonication is recommended.
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Keywords | UNC2025 | Inhibitor | inhibit | FLT3 | leukemia | CD135 | Fms like tyrosine kinase 3 | acute | Cluster of differentiation antigen 135 | cancer | MERTK |
Inhibitors Related | Gilteritinib | Fedratinib | Bemcentinib | Nintedanib | Sunitinib | Sunitinib Malate | Sorafenib | Tandutinib | Pexidartinib | KW-2449 | Sorafenib tosylate | Cabozantinib S-malate |
Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Angiogenesis related Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |