Tyrosine kinase-IN-1

• CAT Number: I010102
• CAS Number: 705946-27-6
• Molecular Formula: C26H28FN5O
• Molecular Weight: 445.53
• Purity: ≥95%
• Synonyms: (3Z)-5-[(1-ethylpiperidin-4-yl)amino]-3-[(3-fluorophenyl)-(5-methyl-1H-imidazol-2-yl)methylidene]-1H-indol-2-one
• InChI: InChI=1S/C26H28FN5O/c1-3-32-11-9-19(10-12-32)30-20-7-8-22-21(14-20)24(26(33)31-22)23(25-28-15-16(2)29-25)17-5-4-6-18(27)13-17/h4-8,13-15,19,30H,3,9-12H2,1-2H3,(H,28,29)(H,31,33)/b24-23-
• InChIKey: DMQYDVBIPXAAJA-VHXPQNKSSA-N
• SMILES: CCN1CCC(CC1)NC2=CC3=C(C=C2)NC(=O)C3=C(C4=CC(=CC=C4)F)C5=NC=C(N5)C

Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.
Tyrosine kinase-IN-1 is from reference (compound 8K)[1].
Tyrosine kinase-IN-1 shows a reasonable PK profile (AUC(0–∞)=1.9, t1/2=4.6 h). It has a favorable oral bioavailability (F=63%) in rats[1].

Reference

[1]. Moon K, et al. The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorganic & Medicinal Chemistry Letters 22 (2012) 4979–4985