TAM Receptor

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.

Tepotinib (EMD-1214063) is an inhibitor of MET tyrosine kinase with potential antineoplastic activity.

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.

NCT-503 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells.

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).

UNC2025 is a potent and orally bioavailable Mer/Flt3 dual inhibitor with IC50 of 0.8/0.74 nM for Mer/Flt3.

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).

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.

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.

Enapotamab is an AXL/UFO-related antibody that can be used to synthesize antibody-drug couplings (Enapotamab Vedotin).

ONO-7475 is an inhibitor with high specificity for anexelekto and MER tyrosine kinase

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).

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.

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].

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.

Dubermatinib (TP0903) is a potent and selective Axl kinase inhibitor.

S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3, blocking cellular phosphorylation of MET, AXL, and FGFRs.

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.

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.

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.

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].

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.

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).

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.

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.

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].

NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.

UNC2250 is an effective and specific Mer inhibitor (IC50=1.7 nM).

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.

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.

RU-301 is a novel pan-tam inhibitor

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.

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.

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.

Bemcentinib (R428) is a selective inhibitor of Axl (IC50: 14 nM) and has been investigated for the treatment of NSCLC.

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.

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].

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.

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).

TAM-IN-2 is an inhibitor of TAM.

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.

XL092 (JUN04542) is an Axl Mer cMet KDR inhibitor for the treatment of Axl and Mer receptor tyrosine kinase- dependent disorders.

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).

G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.