TAM Receptor Inhibitor

Axl-IN-22 is a selective, orally active dual inhibitor of AXL/MER, with IC₅₀ values of 13 nM and 10 nM, respectively. Axl-IN-22 functionally inhibits AXL kinase activity, including ligand-independent autophosphorylation, and blocks the downstream PI3K/AKT signaling pathway, with excellent selectivity over TYRO3, IGF1R and INSR. Axl-IN-22 inhibits tumor growth in vivo and produces a synergistic effect when combined with anti-PD-1 antibody. Axl-IN-22 can be used in studies related to malignant tumors, leukemia, colon cancer and non-small cell lung cancer.

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.

MerTK-IN-1 (compund 31) is a MerTK inhibitor with in vivo target binding ability.

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.

MerTK-IN-2 (compound 15f) is an orally active MerTK inhibitor with an IC₅₀ of 37.5 nM. MerTK-IN-2 can induce apoptosis. MerTK-IN-2 has antitumor activity with IC₅₀ values of 1.79, 18.32, and 2.18 μM for human ovarian cancer cells A2780, breast cancer cells MDA-MB-231, and colon cancer cells HCT116, 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.

R916562 is an orally active and selective Axl/VEGF-R2 inhibitor with IC₅₀s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis.

AXL-IN-14 is a potent and orally active AXL inhibitor with an IC₅₀ value of 0.8 nM. AXL-IN-14 inhibits Gas6/AXL-mediated cell migration and invasion. AXL-IN-14 decreases the expression of p-AXL and p-AKT proteins. AXL-IN-14 shows anti-tumor activity.

Axl-IN-5 (compound 1) is a AXL inhibitor with an IC₅₀ of 283 nM. Axl-IN-5 has anticancer effects.

(Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC).

Protein kinase inhibitor 10 is a protein kinase inhibitor with IC₅₀ values of 28.9, 13.6, and 2.41 μM for TAM receptor, FAK, and KIT, respectively. Protein kinase inhibitor 10 can inhibit abnormal and excessive cell proliferation, showing promise for research in cancer therapy.

Denfivontinib (G-749) hydrochloride is an AXL inhibitor that has synergistic antitumor effects with the PD-1 inhibitor Pembrolizumab (HY-P9902). Denfivontinib can enhance the NOD-like receptor pathway, thereby promoting the formation of the NLRP3 inflammasome.

Ningetinib Tosylate (Standard) is the analytical standard of Ningetinib Tosylate (HY-107145). This product is intended for research and analytical applications. Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine K_inase inhibitor (TK_i) with IC₅₀s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.

SLC-391 is an orally active AXL kinase inhibitor with an IC₅₀ of 9.6 nM against AXL kinase. SLC-391 inhibits Gas6-induced AXL-dependent phosphorylation of Akt. SLC-391 inhibits SARS-CoV-2 infection, entry and replication in cells. SLC-391 suppresses cancer cell proliferation. SLC-391 inhibits tumor growth in mouse solid tumor xenograft models. SLC-391 can be used for the research of COVID-19, influenza virus infection, triple-negative breast cancer, chronic myeloid leukemia and non-small cell lung cancer.

CEP-40783 (Standard) is the analytical standard of CEP-40783 (HY-100946). This product is intended for research and analytical applications. CEP-40783 is a potent, selective and orally available inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively.

Ningetinib (Standard) is the analytical standard of Ningetinib (HY-107145A). This product is intended for research and analytical applications. Ningetinib is a potent, orally bioavailable small molecule tyrosine K_inase inhibitor (TK_i) with IC₅₀s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.

Gilteritinib hemifumarate (Standard) is the analytical standard of Gilteritinib hemifumarate. This product is intended for research and analytical applications. Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.

ER-851 is a selective AXL inhibitor with oral activity with IC₅₀ of 100 nM. ER-851 has antitumor activity.