| Name | AXL-IN-13 |
| Description | 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. |
| In vitro | 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] |
| In vivo | 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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 6.33 mg/mL (10 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (1.58 mM), Sonication is recommended.
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| Keywords | TGFβ1 | TGF-β/Smad | TGFβ | TGFbeta/Smad | TGF-beta | TGFbeta | TGF-b/Smad | TGFb | TAMReceptor | TAM Receptor | Smad | PDGFR | FLT3 | AXL |
| Inhibitors Related | Gilteritinib | Sunitinib | Nintedanib | Regorafenib monohydrate | Imatinib Mesylate | Sorafenib | Hydrochlorothiazide | Regorafenib | Pirfenidone | A 83-01 | Pazopanib | Axitinib |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Anti-Ovarian Cancer Compound Library | Angiogenesis related Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Fluorochemical Library | TGF-beta/Smad Compound Library | Anti-Cancer Active Compound Library |
United States
