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TAM Receptor

The TAM receptors—Tyro3, Axl, and Mer—comprise a unique family of receptor tyrosine kinases,Their regulatory roles are prominent in the mature immune, reproductive, hematopoietic, vascular, and nervous systems. The TAMs and their ligands—Gas6 and Protein S—are essential for the efficient phagocytosis of apoptotic cells and membranes in these tissues.

Bemcentinib
T62691037624-75-1
Bemcentinib (R428) is a selective inhibitor of Axl (IC50: 14 nM) and has been investigated for the treatment of NSCLC.
  • $34
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gilteritinib
T44091254053-43-4
Gilteritinib (ASP2215) is a potent inhibitor of FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preclinical studies, gilteritinib demonstrated strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 clinical trials for acute myeloid leukemia.
  • $34
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Tepotinib
T61211100598-32-0
Tepotinib (EMD-1214063) is a c-MET tyrosine kinase inhibitor (IC50=3 nM) that is selective, orally active, and ATP-competitive. Tepotinib has antitumor effect and is used in the treatment of non-small cell lung cancer.
  • $35
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Cabozantinib
T2586849217-68-1
Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035 1.3 4.6 7 11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.
  • $39
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2-D08
T7379144707-18-6
2-D08 is a synthetic flavone that inhibits sumoylation, also inhibits Axl with an IC50 of 0.49 nM.2-D08 showed anti-aggregatory and neuroprotective effect.
  • $52
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UNC2025
T70071429881-91-3
UNC2025 (mrx-6313)(IC50 of 0.74 nM and 0.8 nM) is a potent and orally bioavailable dual MER FLT3 inhibitor. UNC-2025 is about 20-fold selectivity higher than Axl and Tyro3.
  • $33
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NCT-503
T42131916571-90-8
NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=2.5 µM) with no activity against other dehydrogenases. NCT-503 has antitumor activity and inhibits the growth of PHGDH-dependent tumors.
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Astragalus polysaccharide
T2S083789250-26-0
Astragalus polysaccharide, a natural product derived from Astragalus propinquus, exhibits anticancer activity and has been shown to be effective in hepatocellular carcinoma (HCC) by inhibiting the M2 polarization of tumor-associated macrophages (TAM).
  • $31
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TAM-IN-2
T130742135642-56-5
TAM-IN-2 is an inhibitor of TAM.
  • $51
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SGI-7079
T69821239875-86-5
SGI-7079 is a new selective Axl inhibitor. SGI-7079 can be a dose-dependent manner inhibited growth of tumors. It is also a potential therapeutic target for EGFR inhibitor resistance.
  • $35
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UNC2250
T19681493694-70-4
UNC2250 is an effective and specific Mer inhibitor (IC50=1.7 nM).
  • $38
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Pralatrexate
T6120146464-95-1
Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.
  • $30
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Gilteritinib hemifumarate
T719731254053-84-3
Gilteritinib hemifumarate (ASP2215 hemifumarate) is a potent ATP-competitive dual FLT3 (IC50: 0.29 nM) and AXL (IC50: 0.73 nM) inhibitor for the treatment of relapsed or refractory FLT3 mutant AML.
  • $34
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DS-1205
T91231855860-24-0
DS-1205 is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205 also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205 can inhibit cell migration in vitro and tumor growth in vivo[1].
  • $108
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sitravatinib
T43491123837-84-2
Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.
  • $47
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Dubermatinib
T20051341200-45-0
Dubermatinib (TP0903) is a potent and selective Axl kinase inhibitor.
  • $30
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Tilvestamab
T767232226775-26-2
Tilvestamab (BGB149) is a humanized antibody targeting AXL with anti-tumor and anti-fibrotic activity, inhibiting Gas6-stimulated AXL activation and tumor progression in 786-0 RCC cells, used in cancer research.
  • $228
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Ningetinib
TQ00211394820-69-9
Ningetinib (CT-053) (CT053PTSA) is an orally bioavailable tyrosine kinase inhibitor with IC50s of <1.0, 1.9 and 6.7 nM for Axl, VEGFR2, and c-Met, respectively.
  • $42
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BMS-777607
T26581196681-44-3
BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3.
  • $57
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Emactuzumab
T767761448221-67-7
Emactuzumab(RG 7155) is a monoclonal antibody against colony-stimulating factor-1 receptor targeting tumor-associated macrophages (TAMs) Emactuzumab has antitumor activity and inhibits activation of colony-stimulating factor 1 receptor (CSF1R) Emactuzumab has a high affinity for CSF-1R with a Ki value of 0.2 nM. Emactuzumab blocks CSF-1R dimerization and can be used to study cancers such as diffuse tenosynovial giant cell tumor (dt-GCT).
  • $328
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Cabozantinib hydrochloride
T51641817759-42-4
Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).
  • $37
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LDC1267
T23111361030-48-9
LDC1267 is a excellently specific TAM(Tyro3, Axl and Mer) kinase inhibitor, for Mer( IC50<5 nM), Tyro3(IC50=8 nM), and Axl(IC50=29 nM).
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BMS 777607
T26991025720-94-8
BMS 777607 (BMS 817378) is a Met-related inhibitor targeting c-Met, Axl, Ron, and Tyro3 with IC50 values of 3.9 nM, 1.1 nM, 1.8 nM, and 4.3 nM, respectively. BMS-777607 has been investigated in basic science research for malignant solid tumors.
  • $30
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S49076
T32741265965-22-7
S49076 is a novel and potent inhibitor of MET, AXL MER, and FGFR1 2 3, effectively blocking cellular phosphorylation of MET, AXL, and FGFRs.
  • $39
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