Glesatinib (MGCD265) is a potent, orally bioavailable, spectrum-selective small molecule inhibitor primarily targeting MET and AXL receptor tyrosine kinases. It exhibits strong activity against MET kinase with an IC₅₀ of 1.7 nM and against AXL with an IC₅₀ of 0.4 nM in biochemical assays. Glesatinib is particularly effective in tumors harboring MET exon 14 skipping mutations or MET amplification, showing selective inhibition of MET-driven cell proliferation in preclinical models. In early-phase clinical trials, Glesatinib demonstrated partial responses in non-small cell lung cancer (NSCLC) patients with MET alterations, confirming its mechanism-based activity. Additionally, it shows minimal off-target kinase inhibition, contributing to its relatively favorable safety profile in early human studies.
MedKoo Cat#: 464760
Name: Glesatinib HCl
CAS#: 2319837-80-2 (HCl)
Chemical Formula: C31H28ClF2N5O3S2
Exact Mass: 0.0000
Molecular Weight: 656.16
Elemental Analysis: C, 56.75; H, 4.30; Cl, 5.40; F, 5.79; N, 10.67; O, 7.31; S, 9.77
The following data is based on the product molecular weight 656.16 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 |
