Axl Inhibitor

UNC8212 is a TAM kinase inhibitor. UNC8212 has potent inhibitory activity against MERTK and AXL (IC₅₀: 1.5 nM and 1.3 nM, respectively), and also inhibits TYRO3 (IC₅₀: 6.7 nM). UNC8212 mediates polypharmacological properties by targeting the structurally diverse "back pocket" region of the TAM kinase family. UNC8212 binds tightly to TAM kinases and potently inhibits MERTK and AXL phosphorylation. UNC8212 has anti-tumor effects and can be used in cancer immunotherapy and tumor cell targeting research.

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.

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

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.

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.

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]} .

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.

NTQ2494 is a potent and orally active AXL kinase inhibitor with an IC₅₀ of 4.89 nM. NTQ2494 inhibits AXL kinase catalytic activity. NTQ2494 suppresses tumor growth in mouse xenograft models. NTQ2494 can be used for the research of advanced hematological malignancies, solid tumors.

Axl-IN-19 (Compound 68) is a selective AXL (a membrane-bound receptor tyrosine kinase) inhibitor (IC₅₀: 5.3 nM; Cellular K_D = 6.8 nM). Axl-IN-19 has favorable rat PK with low clearance and moderate bioavailability. Axl-IN-19 can be used for cancer research.

Axl-IN-16 is a dual inhibitor of Axl/HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 inhibits hypoxia-inducible factor activity and receptor tyrosine kinase expression.

Axl-IN-8 (NO.1) is a potent AXL inhibitor, with an IC₅₀ of <1 nM. Axl-IN-8 also inhibits c-MET, with an IC₅₀ of 1-10 nM. Axl-IN-8 shows anti-proliferative activity against BaF3/TEL-AXL, MKN45, and EBC-1 cells, with IC₅₀ values of <10, 226.6 and 120.3 nM, respectively.

Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC₅₀ of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases.