Axl-IN-21

SKU: orb3174553

Description

Axl-IN-21 is an orally bioavailable selective AXL inhibitor with a Kd of 2.7 nM and an IC50 of 4.0 nM. It demonstrates strong inhibitory activity against various cancer-related kinases while maintaining kinase selectivity, including Mer (Kd = 1.4 nM), DDR1 (IC50 = 22.2 nM), HIPK4 (Kd = 11.0 nM), and LOK (Kd = 10 nM). By blocking the AXL/STAT3/ABCG1 signaling pathway induced by GAS6 from tumor-associated fibroblasts, Axl-IN-21 can overcome tumor microenvironment-driven resistance, restore chemotherapy sensitivity, and inhibit drug efflux. In MDA-MB-231 cells, it inhibits TGF-β1-induced epithelial-mesenchymal transition, cell migration, and invasion. Axl-IN-21 exhibits no significant toxicity to non-cancer cells and is relevant for research in triple-negative breast cancer and gastric cancer.

Research Area

Pharmacology & Drug Discovery, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1958081-87-2
• MW: 542.57
• Formula: C₃₀H₂₇FN₄O₅
• SMILES: O=C(NC1=CC=C(OC2=NC=NC=3C=C(OC)C(OC)=CC23)C(F)=C1)C=4C(=O)C5=CC(=CC=C5N(C4C)C)CC
• Target: TGF-beta/Smad,Hedgehog/Smoothened,Discoidin Domain Receptor (DDR),TAM Receptor

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

TGF-beta/Smad,Hedgehog/Smoothened,Discoidin Domain Receptor (DDR),TAM Receptor