AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 of 1.6 nM and a Kd of 0.26 nM. It exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion.

Axl:1.6 nM, PDGFRβ:2.3 nM (Kd)

AXL-IN-13 (Compound 6li) inhibits Ba/F3-TEL-AXL cell proliferation with an IC50 of 4.7 nM (as determined by ELISA).[1]
AXL-IN-13 (0-500 nM; 6 hours) inhibits AXL phosphorylation in MDA-MB-231 and 4T1 cells.[1]
AXL-IN-13 also shows binding affinity for CSF1R, FLT1/3/4, KLT, PDGFRB, TIE2.[1]
AXL-IN-13 (0-3 μM; 3 days) blocks TGF-β1 (10 ng/mL)-induced EMT in MDA-MB-231 cells.[1]
AXL-IN-13 (0-3 μM; 24 hours) inhibits TGF-β1 (10 ng/mL)-induced migration and invasion of MDA-MB-231 cells.[1]

AXL-IN-13 (Compound 6li) (50 or 100 mg/kg; p.o.; 14 days; Xenograft model derived from highly metastatic 4T1 cells) inhibits 4T1 tumor growth and metastasis.[1]
AXL-IN-13 (25 mg/kg; oral; Xenograft model derived from highly metastatic 4T1 cells) shows a good PK curve, 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]