axl

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.

Axl-IN-9 is a potent inhibitor of AXL (IC50: 26 nM) with excellent transmembrane properties.Axl-IN-9 exhibits good pharmacokinetic properties in animals.Axl-IN-9 can be used to study proliferative, autoimmune, allergic, transplant rejection, inflammatory, cancer or other mammalian diseases.

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-11 is a potent inhibitor of AXL. Axl-IN-11 can be used to study proliferative diseases, allergic diseases, autoimmune diseases, inflammatory diseases, cancer, transplant rejection, viral infectious diseases or other mammalian diseases.

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-5 (compound 1) is an AXL inhibitor with an IC50 of 283 nM, demonstrating anticancer activity.

Axl/Mer-IN-1 is a compound that functions as an inhibitor for Axl/Mer receptor tyrosine kinase (Axl/Mer RTK) and CSF1R, exhibiting dissociation constants (Kds) of less than 0.1 μM.

Axl-IN-3 is a selective, potent and orally active inhibitor of AXL kinase (IC50: 41.5 nM) and has a low inhibitory effect on other kinases.

Axl-IN-4 (Compound 24) is an AXL kinase inhibitor with an IC50 of 28.8 μM [1].

Axl-IN-8 (NO.1) is a potent AXL inhibitor (IC50 < 1 nM) and also inhibits c-MET (IC50: 1-10 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].

PROTAC Axl Degrader 1 is a potent and selective compound with an IC50 of 0.92 µM, exhibiting in vitro anti-proliferative and anti-migratory activities, and inducing mehuosis [1].

Axl-IN-10 is a potent inhibitor of AXL (IC50: 5 nM).Axl-IN-10 has good pharmacokinetic properties in animals and excellent transmembrane properties.Axl-IN-10 can be used to study proliferative, allergic, autoimmune, inflammatory, transplant rejection, cancer or other mammalian diseases.

Axl-IN-12 is a potent inhibitor of AXL. Axl-IN-12 can be used to study proliferative, allergic, autoimmune, inflammatory, cancer, transplant rejection, viral infectious diseases or other mammalian diseases.

PROTAC Axl Degrader 2, a potent and selective PROTAC Axl degrader, demonstrates an IC50 of 1.61 µM. It exhibits anti-proliferative and anti-migratory activities in vitro and induces mehuosis [1].

Axl-IN-7 is a potent inhibitor of AXL. Axl-IN-7 can be used to study Axl-related diseases such as cancer (e.g., acute myeloid leukemia, breast cancer, melanoma, pancreatic cancer, and glial tumors), immune system disorders, kidney disease, and cardiovascular disease.

Axl-IN-6 is an orally active inhibitor of AXL. Axl-IN-6 demonstrated good tolerance and significant inhibition of tumor growth in the MV-4-11 subcutaneous xenograft tumor model.

Picropodophyllotoxin (AXL 1717) is a cyclolignan alkaloid found in the mayapple plant family (Podophyllum peltatum), and a small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF1R) with potential antineoplastic activity. Picropodophyllotoxin (AXL 1717) specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast/stem cell growth factor (KIT). This agent shows potent activity in the suppression o f tumor cell proliferation and the induction of tumor cell apoptosis. IGF1R, a receptor tyrosine kinase overexpressed in a variety of human cancers, plays a critical role in the growth and survival of many types of cancer cells.

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.

Trastuzumab deruxtecan (T-DXd) is an antibody-activated molecule coupling (ADC) with anticancer and antitumour activity.Trastuzumab deruxtecan has been shown to have an ameliorative effect in HER2-positive breast and gastric cancers.

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.

Cabozantinib S-malate (XL184) is the s-malate salt form of cabozantinib, an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity.

3-Hydroxymandelic Acid is a metabolite of Phenylephrine. 3-Hydroxymandelic Acid is a metabolite of Phenylephrine, which is an α-receptor agonist.

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).

UNC 569 hydrochloride is a reversible and ATP-competitive inhibitor of Mer with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC 569 hydrochloride inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC 569 hydrochloride can be used in studies about acute lymphoblastic leukemia and atypical teratoid/rhabdoid tumors.

UNC1062 is a highly selective tyrosine kinase inhibitor that specifically targets MERTK. This compound effectively suppresses MERTK-mediated downstream signaling, induces apoptosis in cell cultures, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. Notably, UNC1062 demonstrates potent inhibition of MERTK kinase activity, with an IC50 of 1.1 nM and a Morrison Ki of 0.33 nM. It also displays specificity within the TAM family, exhibiting IC50 values of 60 nM for TYRO3 and 85 nM for AXL [1].

Axltide, based on the mouse Insulin receptor substrate 1 (amino acid 979-989), has a peptide sequence of KKSRGDYMTMQIG.

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.

Bemcentinib (R428) is a selective inhibitor of Axl (IC50: 14 nM) and has been investigated for the treatment of NSCLC.

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

Picropodophyllin (Picropodophyllin (PPP)) (PPP) is a specific IGF-1R inhibitor (IC50: 1 nM). Picropodophyllin specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast stem cell growth factor (KIT).

Ningetinib (CT-053) (CT053PTSA) is an orally bioavailable tyrosine kinase inhibitor with IC50s of <1.0, 1.9 and 6.7 nM for Axl, VEGFR2, and c-Met, respectively.

SNS-314 Mesylate (SNS-314) is an effective and specific Aurora A/B/C inhibitor (IC50: 9/31/3 nM). It is less inhibition of Trk A/B, Fms, Flt4, c-Raf, Axl, and DDR2.

SGI-7079 is a new selective Axl inhibitor. SGI-7079 can be a dose-dependent manner inhibited growth of tumors. It is also a potential therapeutic target for EGFR inhibitor resistance.

Dubermatinib (TP0903) is a potent and selective Axl kinase inhibitor.

UNC2541 is a potent and specific inhibitor of Mer tyrosine kinase (MerTK), binding in the MerTK ATP pocket (IC50: 4.4 nM) and inhibiting phosphorylated MerTK (pMerTK) with an EC50 of 510 nM.

BMS 777607 (BMS 817378) is a Met-related inhibitor targeting c-Met, Axl, Ron, and Tyro3 with IC50 values of 3.9 nM, 1.1 nM, 1.8 nM, and 4.3 nM, respectively. BMS-777607 has been investigated in basic science research for malignant solid tumors.

ONO-7475 is an inhibitor with high specificity for anexelekto and MER tyrosine kinase

RIPK1-IN-7 is a potent and selective inhibitor of RIPK1 (Kd of 4 nM and enzymatic IC50 of 11 nM), exhibiting excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model.

Glumetinib (SCC244) is a novel potent and selective inhibitor of c-Met kinase (IC50: 0.42 nM).

Ningetinib Tosylate is an orally bioavailable tyrosine kinase inhibitor with IC50s of <1.0, 1.9 and 6.7 nM for Axl, VEGFR2, and c-Met, respectively.

UNC569 (UNC 569) is a selective inhibitor of URAT1, a transporter in the kidney that regulates uric acid excretion from the body. It is also a selective uric acid re-absorption inhibitor. UNC569 could normalize the amount of uric acid excreted by gout patients previously classified as under-excretors.

TAM-IN-2 is an inhibitor of TAM.

XL092 (JUN04542) is an Axl Mer cMet KDR inhibitor for the treatment of Axl and Mer receptor tyrosine kinase- dependent disorders.

LDC1267 is a excellently specific TAM(Tyro3, Axl and Mer) kinase inhibitor, for Mer( IC50<5 nM), Tyro3(IC50=8 nM), and Axl(IC50=29 nM).

CEP-40783 (RXDX-106) is an effective, specific and orally active AXL c-Met inhibitor (IC50: 7 12 nM). It also inhibits MER and TYRO3 (IC50: 29 19 nM).

UNC2881 is a specific Mer tyrosine kinase inhibitor (IC50: 4.3 nM). It is about 83- and 58-fold higher selectivity than Axl and Tyro3, respectively.

RU-301 is a novel pan-tam inhibitor

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.