axl

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.

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.

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.

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].

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.

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).

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.

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

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.

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

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).

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.

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