Axl
Axl is a TAM receptor tyrosine kinase activated by GAS6, and TAM receptors support apoptotic-cell recognition, efferocytosis, immune regulation, tissue homeostasis, and cancer-related signaling[1][2]. Mechanistically, Axl participates in ligand-induced TAM activation with TYRO3 and MERTK, but each receptor shows distinct activation patterns with GAS6, PROS1, apoptotic cells, phosphatidylserine vesicles, and enveloped virus[3]. In cancer models, Axl activation stimulates MAPK, AKT, and FAK pathways, while Axl inhibition or knockdown reduces tumor growth, migration, colony formation, and chemoresistance in NSCLC and neuroblastoma[2][4]. In inflammatory disease models, AXL/MERTK inhibition protected against pancreatic necrosis by limiting CXCL2-related neutrophil infiltration, whereas soluble Axl increased in lupus nephritis and multiple sclerosis lesions, indicating disease-linked dysregulation of GAS6-TAM signaling[5][6][7]. Compared with MERTK, Axl showed stronger effects on chemosensitivity in NSCLC, distinct ligand-response behavior among TAM isoforms, and critical roles with TYRO3 in GPVI-mediated platelet activation[3][2][8]. For experimental applications, Axl inhibitors, soluble TAM domains, and antagonist or agonist antibodies provide tools to test TAM signaling, immune regulation, apoptosis, and therapeutic sensitization[3][5][9].
References:
- [1]. Zhou L, et al. Tyro3, Axl, Mertk receptor-mediated efferocytosis and immune regulation in the tumor environment. Int Rev Cell Mol Biol. 2021;361:165-210. [Content Brief]
- [2]. Linger RM, et al. Mer or Axl receptor tyrosine kinase inhibition promotes apoptosis, blocks growth and enhances chemosensitivity of human non-small cell lung cancer. Oncogene. 2013 Jul 18;32(29):3420-31. [Content Brief]
- [3]. Tsou WI, et al. Receptor tyrosine kinases, TYRO3, AXL, and MER, demonstrate distinct patterns and complex regulation of ligand-induced activation. J Biol Chem. 2014 Sep 12;289(37):25750-63. [Content Brief]
- [4]. Li Y, et al. Inhibition of Mer and Axl receptor tyrosine kinases leads to increased apoptosis and improved chemosensitivity in human neuroblastoma. Biochem Biophys Res Commun. 2015 Feb 13;457(3):461-6. [Content Brief]
- [5]. Bao J, et al. AXL and MERTK receptor tyrosine kinases inhibition protects against pancreatic necrosis via selectively limiting CXCL2-related neutrophil infiltration. Biochim Biophys Acta Mol Basis Dis. 2022 Dec 1;1868(12):166490. [Content Brief]
- [6]. Bellan M, et al. Increased plasma levels of Gas6 and its soluble tyrosine kinase receptors Mer and Axl are associated with immunological activity and severity of lupus nephritis. Clin Exp Rheumatol. 2021 Jan-Feb;39(1):132-138. [Content Brief]
- [7]. Weinger JG, et al. Up-regulation of soluble Axl and Mer receptor tyrosine kinases negatively correlates with Gas6 in established multiple sclerosis lesions. Am J Pathol. 2009 Jul;175(1):283-93. [Content Brief]
- [8]. Zhou J, et al. Gas6 Receptors, Tyro3, Axl and Mer, Differentially Participate in Glycoprotein VI-Mediated Platelet activation.
- [9]. Ali SR, et al. Nerve Density and Neuronal Biomarkers in Cancer. Cancers (Basel). 2022 Oct 1;14(19):4817. [Content Brief]
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Axl Related Products (69)
Related Products (69)
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NTQ2494
0 ImagesCat. No.: HY-183774CAS No.: 2750027-59-7
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Axl-IN-19
0 ImagesCat. No.: HY-176204CAS No.: 2870696-46-9
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Axl-IN-8
0 ImagesCat. No.: HY-147575CAS No.: 2231424-62-5Axl-IN-8 (NO.1) is a potent AXL inhibitor, with an IC50 of <1 nM. Axl-IN-8 also inhibits c-MET, with an IC50 of 1-10 nM. Axl-IN-8 shows anti-proliferative activity against BaF3/TEL-AXL, MKN45, and EBC-1 cells, with IC50 values of <10, 226.6 and 120.3 nM, respectively.
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Anticancer agent 109
0 ImagesCat. No.: HY-149092CAS No.: 2097497-16-8Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models.
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Axl-IN-3
0 ImagesCat. No.: HY-144706CAS No.: 2783991-34-2Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC50 of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases.
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R916562
0 ImagesCat. No.: HY-104075CAS No.: 1037798-41-6R916562 is an orally active and selective Axl/VEGF-R2 inhibitor with IC50s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis.
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AXL-IN-14
0 ImagesCat. No.: HY-152075CAS No.: 2947506-65-0AXL-IN-14 is a potent and orally active AXL inhibitor with an IC50 value of 0.8 nM. AXL-IN-14 inhibits Gas6/AXL-mediated cell migration and invasion. AXL-IN-14 decreases the expression of p-AXL and p-AKT proteins. AXL-IN-14 shows anti-tumor activity.
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Axl-IN-5
0 ImagesCat. No.: HY-146596CAS No.: 2642224-24-4Axl-IN-5 (compound 1) is a AXL inhibitor with an IC50 of 283 nM. Axl-IN-5 has anticancer effects.
