AXL-IN-13

• CAT Number: I042460
• CAS Number: 2376928-82-2
• Molecular Formula: C34H41FN6O5
• Molecular Weight: 632.72
• Purity: ≥95%
• Synonyms: N-cyclohexyl-3-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyanilino]-1-methylpyrazole-4-carboxamide
• InChI: InChI=1S/C34H41FN6O5/c1-40-22-26(34(42)38-23-7-4-3-5-8-23)33(39-40)37-24-9-10-30(27(35)19-24)46-29-11-12-36-28-21-32(31(43-2)20-25(28)29)45-16-6-13-41-14-17-44-18-15-41/h9-12,19-23H,3-8,13-18H2,1-2H3,(H,37,39)(H,38,42)
• InChIKey: QBRQTJMZEYORSP-UHFFFAOYSA-N
• SMILES: CN1C=C(C(=N1)NC2=CC(=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OCCCN5CCOCC5)OC)F)C(=O)NC6CCCCC6

AXL-IN-13 is a potent and orally active AXL inhibitor (IC50: 1.6 nM, Kd: 0.26 nM). AXL-IN-13 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion[1].
AXL-IN-13 (compound 6li) inhibits Ba/F3-TEL-AXL cell proliferation with an IC50 of 4.7 nM (determined by ELISA)[1].
AXL-IN-13 also shopws binding affinities against CSF1R, FLT1/3/4, KLT, PDGFRB, TIE2[1].
AXL-IN-13 (0-500 nM, 6 h) inhibits the phosphorylation of AXL in MDA-MB-231 and 4T1 cells[1].
AXL-IN-13 (0-3 μM, 3 days) blocks EMT induced by TGF-β1 (10 ng/mL) in MDA-MB-231 cells[1].
AXL-IN-13 (0-3 μM, 24 h) suppresses MDA-MB-231 cell migration and invasion induced by TGF-β1 (10 ng/mL)[1].
AXL-IN-13 (compound 6li) (50 or 100 mg/kg, p.o, 14 days) inhibits 4T1 tumor growth and metastasis[1].
AXL-IN-13 (25 mg/kg, p.o.) displays reasonable PK profiles with an AUC of 8410.21 ng/mL•h, a T1/2 value of 4.22 h, and an oral bioavailability (F) of 14.4%[1].

Reference

[1]. Chan S, et al. Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors. J Med Chem. 2022 Nov 24;65(22):15374-15390.
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