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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.

  • Gilteritinib
    T44091254053-43-4
    Gilteritinib (ASP2215) is a potent inhibitor at the FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preClinicalal studies, gilteritinib showed strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 Clinicalal trials for acute myeloid leukemia.
    • $34
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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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  • Tepotinib
    T61211100598-32-0
    Tepotinib (EMD-1214063) is an inhibitor of MET tyrosine kinase with potential antineoplastic activity.
    • $43
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  • NCT-503
    T42131916571-90-8
    NCT-503 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells.
    • $35
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  • Astragalus Polysacharin
    T2S0837
    2-(Chloromethyl)-4-(4-nitrophenyl)thiazole is a natural product derived from Astragalus propinquus.2-(Chloromethyl)-4-(4-nitrophenyl)thiazole exhibits anticancer activity. 2-(Chloromethyl)-4-(4-nitrophenyl)thiazole possesses anticancer activity and has been shown to be active in hepatocellular carcinoma (HCC) by inhibiting the M2 polarization of tumor-associated macrophages (TAM).
    • $42
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  • UNC2025 2HCl (1429881-91-3(free base))
    T4419
    UNC2025 is a potent and orally bioavailable Mer/Flt3 dual inhibitor with IC50 of 0.8/0.74 nM for Mer/Flt3.
    • $51
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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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  • UNC 569 hydrochloride
    T21302L
    UNC 569 hydrochloride is a reversible and ATP-competitive inhibitor of Mer with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC 569 hydrochloride inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC 569 hydrochloride can be used in studies about acute lymphoblastic leukemia and atypical teratoid/rhabdoid tumors.
    • $30
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  • AXL-IN-13
    T733002376928-82-2In house
    AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 value of 1.6 nM and a Kd value of 0.26 nM.AXL-IN-13 exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT) and inhibits cancer cell migration and invasion.
    • $79
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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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  • 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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  • 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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  • 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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  • Enapotamab
    T768641912423-61-0
    Enapotamab is an AXL/UFO-related antibody that can be used to synthesize antibody-drug couplings (Enapotamab Vedotin).
    • $263
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  • Ningetinib Tosylate
    TQ00411394820-77-9
    Ningetinib Tosylate 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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  • 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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  • Axl-IN-16
    T79969
    Axl-IN-16, a dual Axl/HIF inhibitor, promotes Flammulina velutipes fruiting body formation and suppresses hypoxia-inducible factor activity along with receptor tyrosine kinase expression [1].
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  • RU-302
    T168061182129-77-6
    RU-302 is a pan inhibitor of TAM Receptor blocking the interface between the TAM Ig1 ectodomain and the Gas6 Lg domain. RU-302 effectively blocks the activation of Gas6-inducible AXL and suppresses lung cancer tumor growth.
    • $60
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  • Dubermatinib
    T20051341200-45-0
    Dubermatinib (TP0903) is a potent and selective Axl kinase inhibitor.
    • $30
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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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  • S49076
    T32741265965-22-7
    S49076 is a novel, potent inhibitor of MET, AXL MER, and FGFR1 2 3, blocking cellular phosphorylation of MET, AXL, and FGFRs.
    • $39
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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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  • 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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  • AXL-IN-15
    T790451954722-22-5
    AXL-IN-15 (cpd391) is a potent inhibitor of Axl, exhibiting both a dissociation constant (K i) and a half-maximal inhibitory concentration (IC50) of less than 1 nanomolar (nM). It is applicable for cancer research [1].
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  • UNC2541
    T172051612782-86-1
    UNC2541 is a potent and Mer tyrosine kinase (MerTK)-specific inhibitor. It also binds in the MerTK ATP pocket (IC50: 4.4 nM). UNC2541 inhibits phosphorylated MerTK (pMerTK; EC50, 510 nM).
    • $42
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  • BMS 777607
    T26991025720-94-8
    BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met/Axl/Ron/Tyro3 (IC50: 3.9/1.1/1.8/4.3 nM). BMS-777607 has been investigated for the basic science of Malignant Solid Tumour.
    • $32
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  • ONO-7475
    T83271646839-59-9
    ONO-7475 is an inhibitor with high specificity for anexelekto and MER tyrosine kinase
    • $57
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  • Sitravatinib malate
    T129252244864-88-6
    Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
    • $1,520
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  • UNC2881
    T26291493764-08-1
    UNC2881 is a specific Mer tyrosine kinase inhibitor (IC50: 4.3 nM). It is about 83- and 58-fold higher selectivity than Axl and Tyro3, respectively.
    • $30
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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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  • RU-301
    T74251110873-99-8
    RU-301 is a novel pan-tam inhibitor
    • $118
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  • NPS-1034
    T69071221713-92-3
    NPS-1034 is a dual Met Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.
    • $32
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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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  • R916562
    T126501037798-41-6
    R916562 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.
    • $1,520
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  • UNC569
    T213021350547-65-7
    UNC569 (UNC 569) is a selective inhibitor of URAT1, a transporter in the kidney that regulates uric acid excretion from the body. It is also a selective uric acid re-absorption inhibitor. UNC569 could normalize the amount of uric acid excreted by gout patients previously classified as under-excretors.
    • $38
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  • S49076 HCl
    T35121265966-31-1
    S49076 HCl (S-49076 Hydrochloride) is an effective inhibitor of MET, AXL/MER, and FGFR1/2/3. S49076 HCl potently blocked cellular phosphorylation of MET, AXL, and FGFRs and inhibited downstream signaling in vitro and in vivo. In cell models, S49076 HCl inhibited the proliferation of MET- and FGFR2-dependent gastric cancer cells blocked MET-driven migration of lung carcinoma cells, and inhibited colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. In tumor xenograft models, a good pharmacokinetic/pharmacodynamic relationship for MET and FGFR2 inhibition following oral administration of S49076 HCl was established and correlated well with impact on tumor growth.
    • $119
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  • XL092
    T90522367004-54-2
    XL092 (JUN04542) is an Axl Mer cMet KDR inhibitor for the treatment of Axl and Mer receptor tyrosine kinase- dependent disorders.
    • $30
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  • AXL-IN-14
    T733102947506-65-0
    AXL-IN-14 is a potent, orally active inhibitor of AXL with an IC50 of 0.8 nM that effectively suppresses Gas6/AXL-mediated cell migration and invasion, reduces the expression of p-AXL and p-AKT proteins, and demonstrates anti-tumor activity [1].
    • $1,820
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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).
    • $30
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  • G-749
    T26201457983-28-6
    G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.
    • $40
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  • TAM-IN-2
    T130742135642-56-5
    TAM-IN-2 is an inhibitor of TAM.
    • $51
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  • Cabozantinib S-malate
    T17971140909-48-3
    Cabozantinib S-malate (XL184) is the s-malate salt form of cabozantinib, an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity.
    • $40
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  • CEP-40783
    T44261437321-24-8
    CEP-40783 (RXDX-106) is an effective, specific and orally active AXL c-Met inhibitor (IC50: 7 12 nM). It also inhibits MER and TYRO3 (IC50: 29 19 nM).
    • $31
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