TAM Receptor

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

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.

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

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.

TAM-IN-2 is an inhibitor of TAM.

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

BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3.

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).

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

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).

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].

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).

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

AXL-IN-15 (cpd391) is a potent Axl inhibitor with a dissociation constant (K i) and half-maximal inhibitory concentration (IC50) of less than 1 nanomolar (nM), suitable for cancer research [1].

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].

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 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.

MerTK Axl-IN-1 (Compound A-910) is a potent and selective dual inhibitor of MerTK Axl, exhibiting IC50 values of 4.2 nM and 8.8 nM in Ba F3 cells, and 0.2 nM and 0.9 nM in HTRF cells, respectively. It effectively inhibits pMerTK in vivo and possesses a long half-life and high oral bioavailability.

MerTK-IN-1 (compound 31) serves as an inhibitor of MerTK, with the capability to bind to the target in vivo.

Protein kinase inhibitor 10 is a protein kinase inhibitor with IC50 values of 28.9 μM, 13.6 μM, and 2.41 μM for TAM receptors, FAK, and KIT, respectively. It can inhibit abnormal and excessive cell proliferation, showing potential for research in the field of cancer treatment.

C-Met Axl-IN-1 (Compound 22a) is an oral, selective type II c-Met Axl inhibitor with IC50 values of 1 nM and 10 nM, respectively. It effectively suppresses tumor cell proliferation, induces cell cycle arrest, and apoptosis (apoptosis), showcasing potent anti-tumor activity.

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.

Mecbotamab vedotin (BA301) is an inhibitory IgG1 antibody that targets human tyrosine kinase receptor AXL and the humanized murine monoclonal BA301 γ1 chain. It can be utilized in the preparation of immunoconjugates for research into cancers expressing the Axl type.