tamreceptor

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.

Bemcentinib (R428) belongs to small molecule inhibitors and is a highly selective oral Axl inhibitor (IC₅₀ = 14 nM) with oral bioavailability and potent cell permeability. This compound effectively inhibits cancer cell migration and invasion, blocks tumor dissemination, and prolongs survival in various tumor models.

AXL-IN-13 is a potent and orally active AXL inhibitor with an IC₅₀ of 1.6 nM and a Kd of 0.26 nM. It exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion.

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.

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.

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.

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

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.

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).

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].

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).

R916562 is an orally active, selective Axl/VEGF-R2 inhibitor with IC₅₀ values of 136 nM and 24 nM, respectively, demonstrating anti-angiogenesis and anti-metastasis properties.

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.

TAM-IN-2 is an inhibitor of TAM.

Merestinib dihydrochloride (LY2801653 dihydrochloride) is an orally available kinase inhibitor with antitumor activity that inhibits MET, AXL, RON, and MKNK1/2, and inhibits the growth of NTRK fusion-carrying tumors.

UNC2541 is a potent and specific inhibitor of Mer tyrosine kinase (MerTK), binding in the MerTK ATP pocket (IC₅₀: 4.4 nM) and inhibiting phosphorylated MerTK (pMerTK) with an EC50 of 510 nM.

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

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

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.

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.

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

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.

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.

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).