UNC8969 macrocyclic dual MERTK/AXL inhibitor(IC50 MERTK = 1.1 nM; IC50 AXL = 5.3 nM). UNC8969 had low-nanomolar activity against both MERTK and AXL and good selectivity over TYRO3 and FLT3. Its target engagement and selectivity were also confirmed by NanoBRET and cell-based MERTK and AXL phosphorylation assays. UNC8969 had excellent pharmacokinetic properties (large AUC and long half-life) and mediated antitumor activity against lung cancer cell lines, indicating its potential as a therapeutic agent.
MedKoo Cat#: 126672
Name: UNC8969
CAS#: 126672
Chemical Formula: C29H41N7O3
Exact Mass: 535.3271
Molecular Weight: 535.69
Elemental Analysis: C, 65.02; H, 7.71; N, 18.30; O, 8.96
The following data is based on the product molecular weight 535.69 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
