Molecular Formula | C28H40N6O |
Molar Mass | 476.66 |
Storage Condition | -20℃ |
In vitro study | In 697 B- ALL cells, UNC-2025 potently inhibited Mer phosphorylation with an IC50 of 2.7 nM. In A549 NSCLC and Molm-14 AML cell lines, UNC-2025 significantly inhibited Mer8 and Flt3 dependent colony formation. In the H2228 and H1299 cell lines, UNC-2025 inhibited the downstream of MERTK oncogenic signals, such as basal and stimulated pAKT and pERK1/2. Of the four NSCLC cell lines, UNC-2025 also induced apoptotic cell death and reduced colony formation. |
In vivo study | In mice bearing 697 acute leukemic tumors, UNC-2025 (3 mg/kg, p.o.) showed good solubility and DMPK performance and elicited potent target inhibition. In mice bearing H2228 or A549 tumors, UNC-2025 (50 mg/kg, p.o.) inhibited tumor growth. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.098 ml | 10.49 ml | 20.979 ml |
5 mM | 0.42 ml | 2.098 ml | 4.196 ml |
10 mM | 0.21 ml | 1.049 ml | 2.098 ml |
5 mM | 0.042 ml | 0.21 ml | 0.42 ml |