Molecular Formula: C22H27FN4O2·C4H6O5 or C26H33FN4O7 (varying representations due to different preparation methods and purity levels).
Molecular Weight: 532.56 or 532.57.
Appearance: Orange-yellow powder, white or light yellow crystalline powder (varying due to preparation method and purity).
Purity: Multiple specifications, such as ≥96%, 98%, 99%, 99.47%, etc.
Physical Properties
Solubility: Easily soluble in DMSO (solubility varies with purity, temperature, etc., e.g., >10 mg/mL for one product, 15 mg/mL for another), difficult to dissolve in ethanol and water.
Melting Point: 189-191°C (approximate, may vary slightly due to preparation conditions).
Inhibits VEGFR2 and PDGFRβ with IC50 values of 80 nM and 2 nM, respectively.
Inhibits KIT and FLT-3 activity, with IC50 values of 211 nM and lower concentrations (e.g., 50 nM for FLT3-ITD).
Shows competitive inhibition against Flk-1 and PDGFRβ (relative to ATP), with Ki values of 9 nM and 8 nM, respectively.
Inhibits FGFR1 tyrosine kinase activity, but with weaker potency, with a Ki value of 0.83 μM.
Biological Activity
Oral Bioavailability: Excellent.
In Vivo Studies: Very effective in many preclinical tumor models and well-tolerated at effective doses. Inhibits the growth of established tumor xenografts.
Mechanism of Action: Blocks the growth, dissemination, migration, and invasion capabilities of tumor cells by inhibiting the activity of multiple RTKs and VEGFRs.
