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Axl-IN-21

CAT: 0804-HY-179535Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-179535Size:1 Each
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Description
Axl-IN-21 is an orally active and selective AXL inhibitor (Kd = 2.7 nM, IC50 = 4.0 nM) . Axl-IN-21 displays kinase selectivity and retains strong activity against cancer-related mul-kinases (Mer with Kd = 1.4 nM, DDR1 with IC50 = 22.2 nM, HIPK4 with Kd = 11.0 nM and LOK with Kd =10 nM) . Axl-IN-21 overcomes tumor microenvironment-driven resistance by blocking CAF-derived GAS6-induced AXL/STAT3/ABCG1 signaling, restoring chemosensitivity and inhibiting drug efflux in gastric cancer (GC) . Axl-IN-21 suppresses TGF-β1-induced epithelial-mesenchymal transition (EMT), migration, and invasion in MDA-MB-231 cells. Axl-IN-21 exhibits no significant cytotoxicity in non-cancerous cells. Axl-IN-21 can be research for triple negative breast cancer and gastric cancer[1] [2] .
CAS Number
1958081-87-2
UNSPSC
12352005
Target
Discoidin Domain Receptor; Hedgehog; TAM Receptor; TGF-β Receptor
Related Pathways
Protein Tyrosine Kinase/RTK; Stem Cell/Wnt; TGF-beta/Smad
Field of Research
Cancer
Smiles
COC1=CC2=C(N=CN=C2OC3=CC=C(C=C3F)NC(C4=C(N(C5=C(C4=O)C=C(C=C5)CC)C)C)=O)C=C1OC
Molecular Formula
C30H27FN4O5
Molecular Weight
542.56
References & Citations
[1]Kim TH, et al. Cancer-associated fibroblast-derived GAS6 increases resistance to chemotherapy through AXL/STAT3/ABCG1 in gastric cancer. Br J Cancer. 2025 Oct 28. doi: 10.1038/s41416-025-03218-|[2]Tan L, et al. 4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors. J Med Chem. 2016 Jul 28;59 (14) :6807-25.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Axl; DDR1; Mer

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