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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UNC1062
0 ImagesUNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC50 of 1.1 nM (Morrison Ki = 0.33 nM). UNC1062 exhibits good selectivity for the TAM family (TYRO3 IC50 = 60 nM, AXL IC50 = 85 nM). UNC1062 exhibits significant anti-proliferative effects and induces apoptosis in various cancer models (such as melanoma, gastric cancer, and acute myeloid leukemia). UNC1062 inhibits multiple pathways, including MAPK/ERK, PI3K/AKT and JAK/STAT and affects the motility of head and neck squamous cell carcinoma (HNSCC) cells through the RhoA signaling pathway. UNC1062 inhibits macrophage efferocytosis, and it suitable for research on atherosclerosis.
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RU-302
0 ImagesRU-302 is a pan TAM inhibitor that blocks the interface between the TAM Ig1 ectodomain and the Gas6 Lg domain. RU-302 effectively blocks Gas6-inducible Axl receptor activation with a low micromolar IC50in cell assays, and suppresses lung cancer tumor growth.
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UNC2881
0 ImagesUNC2881 is an orally active and specific Mer kinase inhibitor, inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. UNC2881 shows additional inhibition against Axl and Tyro with IC50s of 360 nM and 250 nM, respectively. UNC2881 potently inhibits collagen-induced platelet aggregation, can be used for pathologic thrombosis research.
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Enapotamab
0 ImagesSynonyms: Anti-AXL/UFO Reference Antibody (enapotamab)Enapotamab (Anti-AXL/UFO Reference Antibody) is an AXL/UFO-related antibody that can be used for synthesis of ADC molecule Enapotamab vedotin (HY-P99921).
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Mecbotamab
0 ImagesSynonyms: BA301Mecbotamab is a humanized IgG1-κ antibody targeting to AXL receptor tyrosine kinase (AXL). Mecbotamab can serves as a conditionally active biologic (CAB), which can be conjugated with MMAE (HY-15162) via a cleavable linker, to form ADC Mecbotamab vedotin (BA3011).
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PF-07265807
0 ImagesCat. No.: HY-147218CAS No.: 2412356-57-9Synonyms: ARRY-067PF-07265807 (ARRY-067) is a kinase inhibitor with primary targets AXL, MERTK, and TYRO3. PF-07265807 acts as an immunomodulator that cross-activates CD8+ T cells by enhancing dendritic cell function. PF-07265807 blocks downstream signal transduction of AXL and MERTK, and inhibits the proliferation and migration of tumor cells with high expression of these two kinases. PF-07265807 is applicable to research related to advanced or metastatic solid tumors, such as colorectal cancer.
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Adrixetinib
0 ImagesSynonyms: Q702Adrixetinib (Q702) is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma.
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PROTAC Axl Degrader 2
0 ImagesCat. No.: HY-144627CAS No.: 3033401-45-2PROTAC Axl Degrader 2 is an orally active and selective AXL PROTAC degrader with dual activities of AXL kinase inhibition and AXL protein degradation. PROTAC Axl Degrader 2 induces cytoplasmic vacuolization, excessive macropinosome production, oncosis, H-Ras activation, and Rac1-dependent non-apoptotic cell death. PROTAC Axl Degrader 2 inhibits the proliferation and migration of cancer cells, and also suppresses the growth of tumor cell xenografts under in vivo conditions. PROTAC Axl Degrader 2 can be used in research related to breast cancer.
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Cabozantinib-d6
0 ImagesSynonyms: XL184-d6; BMS-907351-d6
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Adrixetinib TFA
0 ImagesCat. No.: HY-152830APurity: 99.26%Synonyms: Q702 TFAAdrixetinib (Q702) TFA is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib TFA acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib TFA increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib TFA upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib TFA shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib TFA is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma.
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Mipasetamab
0 ImagesMipasetamab is an IgG1κ antibody targeting to AXL, a tyrosine kinase receptor and an TAM Receptor. Mipasetamab involves in synthesis of ADCT-601 (Mipasetamab uzoptirine), an AXL-targeted antibody-drug conjugate (ADC). ADCT-601 has anti-tumor activity.
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Ladarutatug
0 ImagesCat. No.: HY-P992116CAS No.: 3075939-11-3
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TL4830031
0 ImagesTL4830031 (compound 8i), a quinolone antibiotic derivatives, is a potent Axl inhibitor with an IC50 value of 26 nM. TL4830031 inhibits the phosphorylation of Axl. TL4830031 inhibits cell invasion and migration. TL4830031 can be used for cancer research.
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AG01
0 ImagesCat. No.: HY-P991664AG01 is a monoclonal antibody against progranulin (GP88). AG01 inhibits triple-negative breast cancer (TNBC) cell proliferation and migration, reduces the expression of phosphorylated protein kinases p-Src, p-AKT, and p-ERK, and reduces the expression of oncogenic proteins such as Axl, c-MET, HIF-1α, and VEGF. AG01 inhibits tumor growth and Ki67 expression in a TNBC xenograft mouse model. AG01 can be used in the research of TNBC and other cancers.
