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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Cabozantinib hydrochloride
0 ImagesCat. No.: HY-13016ACAS No.: 1817759-42-4Synonyms: XL184 hydrochloride; BMS-907351 hydrochlorideCabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.
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Axl-IN-6
0 ImagesCat. No.: HY-146615CAS No.: 2642224-22-2Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model.
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UNC8212
0 ImagesCat. No.: HY-173400UNC8212 is a TAM kinase inhibitor. UNC8212 has potent inhibitory activity against MERTK and AXL (IC50: 1.5 nM and 1.3 nM, respectively), and also inhibits TYRO3 (IC50: 6.7 nM). UNC8212 mediates polypharmacological properties by targeting the structurally diverse "back pocket" region of the TAM kinase family. UNC8212 binds tightly to TAM kinases and potently inhibits MERTK and AXL phosphorylation. UNC8212 has anti-tumor effects and can be used in cancer immunotherapy and tumor cell targeting research.
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Axl ligand-1
0 ImagesCat. No.: HY-184184CAS No.: 3033401-32-7Axl ligand-1 is a highly selective ligand for AXL kinase, exhibiting higher selectivity for AXL over 72 human kinases. Axl ligand-1 serves as a Ligand for Target Protein for PROTAC, which is applied to develop PROTAC degraders with anti-tumor activity, such as PROTAC Axl Degrader 1 (HY-144624). Axl ligand-1 is applicable to breast cancer-related research.
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Axl-IN-9
0 ImagesCat. No.: HY-147576CAS No.: 2487649-73-8Axl-IN-9 (Example 10) is a potent AXL inhibitor, with an IC50 of 26 nM. Axl-IN-9 has excellent transmembrane properties. Axl-IN-9 exhibits excellent pharmacokinetic properties in an animal body. Axl-IN-9 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals.
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Axl-IN-11
0 ImagesCat. No.: HY-147578CAS No.: 2758688-17-2Axl-IN-11 (Example 1) is a potent AXL inhibitor. Axl-IN-11 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals.
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PROTAC Axl Degrader 1
0 ImagesCat. No.: HY-144624CAS No.: 3033401-47-4PROTAC Axl Degrader 1 is an orally active PROTAC degrader targeting the AXL receptor tyrosine kinase, with an IC50 of 0.92 μM against human targets. PROTAC Axl Degrader 1 induces cytoplasmic vacuolization, methuosis (macropinocytosis-induced cell death), excessive macropinosome production, and Rac1 activation. PROTAC Axl Degrader 1 inhibits the proliferation and migration of cancer cells. PROTAC Axl Degrader 1 can be used in breast cancer-related research.
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TAM-IN-1
0 ImagesCat. No.: HY-122601CAS No.: 1454847-05-2
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Axl-IN-4
0 ImagesCat. No.: HY-144708CAS No.: 1176456-11-3Axl-IN-4 (Compound 24) is an AXL kinase inhibitor with an IC50 of 28.8 μM.
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Axl-IN-17
0 ImagesCat. No.: HY-162085CAS No.: 3048409-80-6Axl-IN-17 (compound 13c) is an orally active, selective AXL inhibitor with an IC50 value of 3.2 nM. Axl-IN-17 reveals antitumor efficacy.
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Axl-IN-10
0 ImagesCat. No.: HY-147577CAS No.: 2487649-61-4Axl-IN-10 (Example 1) is a potent AXL inhibitor, with an IC50 of 5 nM. Axl-IN-10 has excellent transmembrane properties.Axl-IN-10 exhibits excellent pharmacokinetic properties in an animal body. Axl-IN-10 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals.
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Bemcentinib (GMP)
0 ImagesCat. No.: HY-15150GCAS No.: 1037624-75-1Synonyms: R428 (GMP); BGB324 (GMP)Bemcentinib (R428) GMP is Bemcentinib (HY-15150) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy.Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer.
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HIV-IN-7
0 ImagesCat. No.: HY-149491CAS No.: 3032472-86-6
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Axl/Mer/CSF1R-IN-1
0 ImagesCat. No.: HY-153012CAS No.: 2394874-60-1Axl/Mer-IN-1 (Compound 1) is an Axl/Mer receptor tyrosine kinase (Axl/Mer RTK) and CSF1R inhibitor with Kds of <0.1 μM.
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Axl-IN-21
0 ImagesCat. No.: HY-179535CAS No.: 1958081-87-2Axl-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] .
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UNC3133
0 ImagesCat. No.: HY-115778CAS No.: 2011034-35-6
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Axl-IN-12
0 ImagesCat. No.: HY-147579CAS No.: 2758062-17-6Axl-IN-12 (Example 2) is a potent AXL inhibitor. Axl-IN-12 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals.
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AXL-IN-15
0 ImagesCat. No.: HY-153441CAS No.: 1954722-22-5
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Axl-IN-7
0 ImagesCat. No.: HY-147574CAS No.: 1770821-83-4Axl-IN-7 (Chemie 22) is a potent AXL inhibitor. Axl-IN-7 can be used for Axl-related diseases research, for example cancers (such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors), renal disease, immune system disorders, and cardiovascular disease.
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Axl-IN-22
0 ImagesCat. No.: HY-184433CAS No.: 2758062-71-2Axl-IN-22 is a selective, orally active dual inhibitor of AXL/MER, with IC50 values of 13 nM and 10 nM, respectively. Axl-IN-22 functionally inhibits AXL kinase activity, including ligand-independent autophosphorylation, and blocks the downstream PI3K/AKT signaling pathway, with excellent selectivity over TYRO3, IGF1R and INSR. Axl-IN-22 inhibits tumor growth in vivo and produces a synergistic effect when combined with anti-PD-1 antibody. Axl-IN-22 can be used in studies related to malignant tumors, leukemia, colon cancer and non-small cell lung cancer.
