TAM Receptor Inhibitor

Axl-IN-9 (Example 10) is a potent AXL inhibitor, with an IC₅₀ of 26 nM. Axl-IN-9 has excellent transmembrane properties. Axl-IN-9 exhibits excellent pharmacokinetic properties in an animal body. Axl-IN-9 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals.

Axl-IN-11 (Example 1) is a potent AXL inhibitor. Axl-IN-11 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals.

TAM-IN-1 (compound 1) is a potent macrocyclic inhibitor of Axl and Mer, with K_is of 130 pM and <50 pM, respectively.

Multi-kinase-IN-1 (Compound 11k) is a potent kinase inhibitor with antitumor activity. Multi-kinase-IN-1 induces cell apoptosis, and can be studied for colorectal cancer.

Axl-IN-4 (Compound 24) is an AXL kinase inhibitor with an IC₅₀ of 28.8 μM.

Anti-GAS6 Antibody (KM5321) is a humanized anti-GAS6 monoclonal antibody. Its isotype control is Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).

Axl-IN-17 (compound 13c) is an orally active, selective AXL inhibitor with an IC₅₀ value of 3.2 nM. Axl-IN-17 reveals antitumor efficacy.

YAP/TAZ-TEAD-IN-2 (Compound 51) is a YAP/TAZ-TEAD inhibitor that inhibits the interaction between YAP/TAZ and TEAD. YAP/TAZ-TEAD-IN-2 suppresses the transcriptional activity of TEAD, with an IC₅₀ of 1.2 nM. YAP/TAZ-TEAD-IN-2 inhibits YAP/TAZ-TEAD target genes expression (Cyr61, CTGF, AXL and Survivin) and breast cancer cell proliferation.

Axl-IN-10 (Example 1) is a potent AXL inhibitor, with an IC₅₀ of 5 nM. Axl-IN-10 has excellent transmembrane properties.Axl-IN-10 exhibits excellent pharmacokinetic properties in an animal body. Axl-IN-10 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals.

SMU-B is the orally active inhibitor for ALK (IC₅₀<0.5 nM), c-ros oncogene 1 (ROS1), c-MET (IC₅₀=1.87 nM) and AXL (IC₅₀=28.9 nM). SMU-B inhibits the proliferation of MKN45, H1993 and H441 with IC₅₀s of 0.02 μM, 1.58 μM and 2.82 μM, respectively. SMU-B exhibits antitumor efficacy in mouse models.

Bemcentinib (R428) GMP is Bemcentinib (HY-15150) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy.Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC₅₀ of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer.

Axl-IN-16 (Compound 4) is a Axl inhibitor. Axl-IN-16 inhibits Axl expression and inhibits the activity of HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 can be isolated from“fruiting liquid (FL)” of Hypholoma lateritium and Hericium erinaceus.

Axl/Mer-IN-1 (Compound 1) is an Axl/Mer receptor tyrosine kinase (Axl/Mer RTK) and CSF1R inhibitor with K_ds of <0.1 μM.

Axl-IN-21 is an orally active and selective AXL inhibitor (K_d = 2.7 nM, IC₅₀ = 4.0 nM). Axl-IN-21 displays kinase selectivity and retains strong activity against cancer-related mul-kinases (Mer with K_d = 1.4 nM, DDR1 with IC₅₀ = 22.2 nM, HIPK4 with K_d = 11.0 nM and LOK with K_d =10 nM). Axl-IN-21 overcomes tumor microenvironment-driven resistance by blocking CAF-derived GAS6-induced AXL/STAT3/ABCG1 signaling, restoring chemosensitivity and inhibiting drug efflux in gastric cancer (GC). Axl-IN-21 suppresses TGF-β1-induced epithelial-mesenchymal transition (EMT), migration, and invasion in MDA-MB-231 cells. Axl-IN-21 exhibits no significant cytotoxicity in non-cancerous cells. Axl-IN-21 can be research for triple negative breast cancer and gastric cancer^{[1] [2]} .

Axl-IN-18 (compound 25c) is a potent and selective type II AXL inhibitor. Axl-IN-18 shows excellent AXL inhibitory activity (IC₅₀=1.1 nM) and 343-fold selectivity over the highly homologous kinase MET in biochemical assays (IC₅₀=377 nM). Axl-IN-18 significantly inhibits AXL-driven cell proliferation, dose-dependently suppresses 4T1 cell migration and invasion, and induces apoptosis. Axl-IN-18 shows noticeable antitumor efficacy in a BaF3/TEL-AXL xenograft model.

C-Met/Axl-IN-1 (Compound 22a) is an orally active and selective type II c-Met/Axl inhibitor with IC₅₀ values of 1 nM and 10 nM, respectively. C-Met/Axl-IN-1 can inhibit proliferation, induce cell cycle arrest and apoptosis of tumor cells. C-Met/Axl-IN-1 has strong anti-tumor activity.

UNC3133 is an orally active, limitedly selective MerTK inhibitor with an IC₅₀ of 3.0 nM. UNC3133 inhibits Axl, Tyro3 and Flt3 kinases, with IC₅₀ values of 17 nM, 31 nM and 6.8 nM, respectively. UNC3133 is applicable to the research of inflammatory diseases and cancers.

Axl-IN-12 (Example 2) is a potent AXL inhibitor. Axl-IN-12 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals.

AXL-IN-15 (cpd391) is a potent Axl inhibitor with both K_i and IC₅₀ <1 nM. AXL-IN-15 can be used for research in cancer.

Axl-IN-7 (Chemie 22) is a potent AXL inhibitor. Axl-IN-7 can be used for Axl-related diseases research, for example cancers (such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors), renal disease, immune system disorders, and cardiovascular disease.