Information UNC2025 HCl UNC2025 HCl is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3. Targets Mer (Cell-free assay); FLT3 (Cell-free assay); Axl (Cell-free assay); Tyro3 (Cell-free assay) 0.74 nM ;0.8 nM; 14 nM; 17 nM 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. 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. 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. In mice bearing H2228 or A549 tumors, UNC-2025 (50 mg/kg, p.o.) inhibits tumor growth.
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UNC2025 HCl
CAS number：2070015-17-5 molecular formula：C28H41ClN6O
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| Chinese alias | - | ||
| English alias | UNC2025 hydrochloride(1r,4r)-4-(2-(butylamino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol hydrochloride | ||
| CAS number | 2070015-17-5 | molecular formula | C28H41ClN6O |
| molecular weight | 513.12 g/mol | Exact mass | ≥99% |
| PSA | 69.500 Ų | logp | 4.96 |
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