Axl Inhibitor

UNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC₅₀ of 1.1 nM (Morrison K_i = 0.33 nM). UNC1062 exhibits good selectivity for the TAM family (TYRO3 IC₅₀ = 60 nM, AXL IC₅₀ = 85 nM). UNC1062 exhibits significant anti-proliferative effects and induces apoptosis in various cancer models (such as melanoma, gastric cancer, and acute myeloid leukemia). UNC1062 inhibits multiple pathways, including MAPK/ERK, PI3K/AKT and JAK/STAT and affects the motility of head and neck squamous cell carcinoma (HNSCC) cells through the RhoA signaling pathway. UNC1062 inhibits macrophage efferocytosis, and it suitable for research on atherosclerosis.

RU-302 is a pan TAM inhibitor that blocks the interface between the TAM Ig1 ectodomain and the Gas6 Lg domain. RU-302 effectively blocks Gas6-inducible Axl receptor activation with a low micromolar IC₅₀in cell assays, and suppresses lung cancer tumor growth.

UNC2881 is an orally active and specific Mer kinase inhibitor, inhibits steady-state Mer kinase phosphorylation with an IC₅₀ value of 22 nM. UNC2881 shows additional inhibition against Axl and Tyro with IC₅₀s of 360 nM and 250 nM, respectively. UNC2881 potently inhibits collagen-induced platelet aggregation, can be used for pathologic thrombosis research.

Enapotamab (Anti-AXL/UFO Reference Antibody) is an AXL/UFO-related antibody that can be used for synthesis of ADC molecule Enapotamab vedotin (HY-P99921).

Mecbotamab is a humanized IgG1-κ antibody targeting to AXL receptor tyrosine kinase (AXL). Mecbotamab can serves as a conditionally active biologic (CAB), which can be conjugated with MMAE (HY-15162) via a cleavable linker, to form ADC Mecbotamab vedotin (BA3011).

Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC₅₀s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.

PF-07265807 (ARRY-067) is a kinase inhibitor with primary targets AXL, MERTK, and TYRO3. PF-07265807 acts as an immunomodulator that cross-activates CD8⁺ T cells by enhancing dendritic cell function. PF-07265807 blocks downstream signal transduction of AXL and MERTK, and inhibits the proliferation and migration of tumor cells with high expression of these two kinases. PF-07265807 is applicable to research related to advanced or metastatic solid tumors, such as colorectal cancer.

UNC4203 is a potent, orally available and highly selective MERTK inhibitor, with IC₅₀s of 1.2 nM, 140 nM, 42 nM and 90 nM for MERTK, AXL, TYRO3 and FLT3, respectively.

Adrixetinib (Q702) is an orally active triple inhibitor against CSF1R, Mer, and Axl, with K_d values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma.

DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC₅₀ of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC₅₀s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo.

Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC₅₀s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.

Cabozantinib-d₆ is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC₅₀s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

AXL-IN-13 is a potent and orally active AXL inhibitor (IC₅₀: 1.6 nM, K_d: 0.26 nM). AXL-IN-13 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion.

Adrixetinib (Q702) TFA is an orally active triple inhibitor against CSF1R, Mer, and Axl, with K_d values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib TFA acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib TFA increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib TFA upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib TFA shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib TFA is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma.

Mipasetamab is an IgG1κ antibody targeting to AXL, a tyrosine kinase receptor and an TAM Receptor. Mipasetamab involves in synthesis of ADCT-601 (Mipasetamab uzoptirine), an AXL-targeted antibody-drug conjugate (ADC). ADCT-601 has anti-tumor activity.

Ladarutatug is a humanized monoclonal antibody targeting Tyrosine-protein kinase receptor UFO. The Ladarutatug antibody isotype is human IgG4κ; the recommended isotype control is Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).

TL4830031 (compound 8i), a quinolone antibiotic derivatives, is a potent Axl inhibitor with an IC₅₀ value of 26 nM. TL4830031 inhibits the phosphorylation of Axl. TL4830031 inhibits cell invasion and migration. TL4830031 can be used for cancer research.

AG01 is a monoclonal antibody against progranulin (GP88). AG01 inhibits triple-negative breast cancer (TNBC) cell proliferation and migration, reduces the expression of phosphorylated protein kinases p-Src, p-AKT, and p-ERK, and reduces the expression of oncogenic proteins such as Axl, c-MET, HIF-1α, and VEGF. AG01 inhibits tumor growth and Ki67 expression in a TNBC xenograft mouse model. AG01 can be used in the research of TNBC and other cancers.

Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC₅₀ values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC₅₀=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.

Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model.