Catalog No.
Product Name
Application
Product Information
Citations
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c-Met inhibitor
BMS-777607 is a MET tyrosine kinase inhibitor that binds to c-Met protein, or HGFR, preventing binding of HGF and disrupting the MET signaling pathway. -
VEGFR inhibitor
XL184 free base (Cabozantinib) is a small molecule designed to inhibit multiple receptor tyrosine kinases, specifically MET and VEGFR2.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Jhe-Cyuan Guo, .et al. , Journal of Clinical Oncology, 2024, May 29
- Feyza Oflaz, .et al. , Cumhuriyet Sci. J., 2023, 44(4): 650-655
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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multiple receptor tyrosine kinases inhibitor
Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases 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.- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
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Axl Inhibitor
R428 is a selective small molecule inhibitor of Axl kinase, which showed activity to blocks tumor spread and prolongs survival in models of metastatic breast cancer.- Ofra Novoplansky, .et al. , J Exp Clin Cancer Res, 2024, Nov 20;43(1):308 PMID: 39567998
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Selective Mer Kinase inhibitor
UNC2250 is a potent and selective Mer Kinase inhibitor.- Hongbo Xu, .et al. , Acta Pharm Sin B, 2024, May;14(5):2247-2262 PMID: 38799631
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FLT3/Axl inhibitor
Gilteritinib is a potent FLT3/AXL inhibitor, which showed potent antileukemic activity against AML with either or both FLT3-ITD and FLT3-D835 mutations.- Mohammad Azhar, .et al. , Blood Adv, 2022, Aug 31 PMID: 36044389
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AXL Inhibitor
TP-0903 is a potent and selective Axl kinase inhibitor with IC50 of 27 nM. -
MET/Axl inhibitor
Glesatinib hydrochloride is an inhibitor of the MET and Axl receptor tyrosine kinase pathways, which drive tumour growth when altered. -
tyrosine kinase inhibitor
Ningetinib is a multi-kinase inhibitor that inhibits c-Met, VEGFR2/KDR, and Axl with IC50s value of 19, 37, and 11 nM, respectively. -
FLT3/AXL inhibitor
Gilteritinib hemifumarate is a potent FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively. -
AXL kinase inhibitor
DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. -
AXL Inhibitor
Axl-IN-20 is a selective AXL inhibitor with a potent IC50 of 5 nM. This orally active compound demonstrates significant anti-tumor activity, particularly against hematological malignancies. It is a valuable tool for research applications aimed at understanding AXL signaling pathways and developing targeted cancer therapies. -
TAM Receptor Inhibitor
TAM-IN-1 is a potent macrocyclic inhibitor targeting TAM receptors Axl and Mer, displaying binding affinities with Kis of 130 pM and <50 pM, respectively. This compound demonstrates significant biological activity in modulating pathways associated with tumor progression and immune evasion. TAM-IN-1 is applicable in research focused on cancer therapeutics and the study of receptor-mediated signaling in the tumor microenvironment. -
TYRO3 Inhibitor
UNC9426 is a highly selective inhibitor of TYRO3, exhibiting an IC50 of 2.1 nM and demonstrating 276-fold and 90-fold selectivity over MERTK and AXL, respectively. This compound effectively reduces platelet aggregation without prolonging bleeding time, and it inhibits TYRO3-mediated processes in both tumor cells and macrophages. With a favorable safety profile, UNC9426 is an invaluable tool for investigating TYRO3-dependent phenotypes, including applications in non-small cell lung cancer (NSCLC) research. -
AXL Inhibitor
Ligritinib is an AXL receptor tyrosine kinase inhibitor that displays oral bioavailability. It effectively inhibits AXL kinase activity, disrupting downstream signaling pathways associated with cancer progression. Ligritinib is particularly relevant in cancer research, and it is often investigated in combination with chemotherapy for the treatment of non-small cell lung cancer (NSCLC). -
MER/AXL Inhibitor
BPR5K230 is a dual inhibitor targeting the receptor tyrosine kinases MER and AXL, exhibiting IC50 values of 4.1 nM and 9.2 nM, respectively. This compound effectively inhibits the proliferation of Ba/F3-MER cells, with an IC50 of 5 nM. In preclinical models, BPR5K230 demonstrates anti-inflammatory and antitumor activities against various cancer cell lines, including 4T1, MDA-MB-231, MC38, and Hepa1-6, as well as favorable pharmacokinetic properties in mice. These attributes make BPR5K230 a valuable tool for research into cancer biology and targeted therapies. -
TAM Receptor Inhibitor
AZ14145845 is a selective inhibitor targeting the TAM receptor kinases Mer and Axl, classified as a type I1/2 dual kinase inhibitor. This compound demonstrates notable in vivo efficacy, making it a valuable tool for research in cancer biology and therapeutic resistance mechanisms. Its selective inhibition of the TAM receptors contributes to the modulation of immune responses and potential enhancement of antitumor activity, serving as a significant asset in studies focused on cancer treatment and immunotherapy. -
Axl Inhibitor
TL4830031 is a potent Axl inhibitor, exhibiting an IC50 value of 26 nM. This compound effectively disrupts Axl phosphorylation, leading to inhibition of cell invasion and migration. TL4830031 is an ideal reagent for cancer research applications, providing valuable insights into tumor biology and potential therapeutic interventions targeting the Axl pathway. -
AXL Inhibitor
Axl-IN-6 is a potent AXL inhibitor that demonstrates significant anti-tumor activity. This orally active compound effectively inhibits tumor growth in the MV-4-11 subcutaneous xenograft model, showcasing its potential for cancer research applications. Axl-IN-6 is well tolerated, making it a suitable candidate for evaluating AXL targeting in therapeutic studies. -
MerTK Inhibitor
MerTK-IN-3 is a selective MerTK inhibitor, demonstrating an IC50 of 21.5 nM for MerTK while maintaining a significantly higher IC50 of 991.3 nM for Tyro3. This compound is suitable for research applications focused on colon cancer, enabling studies into MerTK's role in tumor progression and potential therapeutic interventions. Its oral bioavailability further enhances its utility in preclinical studies. -
AXL Inhibitor
Axl-IN-9 is a potent inhibitor of AXL, exhibiting an IC50 of 26 nM. This compound demonstrates excellent transmembrane and pharmacokinetic properties, making it suitable for in vivo studies. Axl-IN-9 is intended for research applications in proliferative diseases, autoimmune disorders, allergic reactions, inflammatory conditions, transplant rejection, cancer, and other related mammalian diseases. -
AXL Inhibitor
Axl-IN-11 is a potent AXL inhibitor that targets the AXL receptor tyrosine kinase. It exhibits significant biological activity in the modulation of cell proliferation and migration, making it useful in the study of various proliferative and autoimmune diseases, as well as in cancer research. Additionally, Axl-IN-11 can be applied in the investigation of allergic, inflammatory, and viral infectious diseases, as well as transplant rejection mechanisms in mammals. -
AXL Inhibitor
Axl-IN-4 is an AXL kinase inhibitor that demonstrates an IC50 of 28.8 μM. This compound specifically targets the AXL receptor tyrosine kinase, which is implicated in multiple cancer pathways and immune responses. Axl-IN-4 is useful for research applications aiming to elucidate the roles of AXL in tumor progression and to explore potential therapeutic strategies against AXL-driven malignancies. -
AXL inhibitor
Axl-IN-17 is a selective AXL inhibitor that demonstrates potent inhibitory activity with an IC50 value of 3.2 nM. This compound exhibits significant antitumor efficacy, making it a valuable tool for research in cancer biology. Axl-IN-17 is suitable for studies focusing on AXL-mediated signaling pathways and their implications in tumor progression and metastasis. -
AXL Inhibitor
Axl-IN-10 is a potent AXL inhibitor with an IC50 of 5 nM, effectively targeting the AXL receptor. This compound exhibits favorable transmembrane and pharmacokinetic properties, enhancing its utility in biological research. Axl-IN-10 is applicable in the study of various proliferative diseases, autoimmune disorders, allergic reactions, inflammatory conditions, transplant rejection, and cancer, making it a valuable tool for researchers exploring these complex pathologies in mammals. -
MerTK Inhibitor
UNC3133 is a selective and orally bioavailable inhibitor of the Mer tyrosine kinase (MerTK), demonstrating an IC50 of 8.1 nM. This compound exhibits preferential inhibition of the TAM receptor family, particularly with approximately sevenfold selectivity for Axl and tenfold selectivity for Tyro3, while also showing comparable activity against Flt3. UNC3133 is applicable in research focused on anti-tumor and anti-infection mechanisms, providing insights into therapeutic strategies targeting these pathways. -
AXL Inhibitor
Axl-IN-12 is a potent AXL inhibitor that selectively targets the AXL receptor tyrosine kinase. It exhibits significant biological activity in regulating cell proliferation and modulating immune responses. Axl-IN-12 is suitable for research applications related to proliferative diseases, autoimmune disorders, allergic responses, inflammation, transplant rejection, various malignancies, and viral infections in mammalian systems. -
Axl Inhibitor
AXL-IN-15 is a highly potent inhibitor of the Axl receptor tyrosine kinase, exhibiting Ki and IC50 values of less than 1 nM. This compound is valuable for research focused on cancer biology, particularly in studies investigating Axl's role in tumor progression and metastasis. AXL-IN-15 can aid in elucidating the molecular mechanisms underlying Axl-mediated signaling pathways and their implications in various malignancies. -
AXL Inhibitor
Axl-IN-7 is a potent inhibitor of the AXL receptor tyrosine kinase. This compound demonstrates significant activity in targeting AXL-mediated signaling pathways, making it valuable for investigating AXL-related diseases, including various cancers such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors. Additionally, Axl-IN-7 has potential applications in research focused on renal diseases, immune system disorders, and cardiovascular conditions. -
MerTK/Axl Inhibitor
MerTK/Axl-IN-1 is a highly selective dual inhibitor targeting MerTK and Axl receptors, demonstrating potent inhibitory activity with IC50 values of 4.2 nM and 8.8 nM in Ba/F3 cells, and 0.2 nM and 0.9 nM in HTRF assays. This compound effectively inhibits phosphorylated MerTK (pMerTK) in vivo, indicating its utility in biological research. With a prolonged half-life and favorable oral bioavailability, MerTK/Axl-IN-1 is suitable for studies in cancer biology and therapeutic development aimed at disruptions in MerTK and Axl signaling pathways. -
AXL Inhibitor
Axl-IN-19 is a selective inhibitor of AXL, a membrane-bound receptor tyrosine kinase, exhibiting an IC50 of 5.3 nM and a cellular KD of 6.8 nM. This compound demonstrates favorable pharmacokinetic properties in rats, characterized by low clearance and moderate bioavailability. Axl-IN-19 is primarily utilized in cancer research to explore the role of AXL signaling in tumor progression and metastasis. -
TAM Receptor Inhibitor
MerTK-IN-1 is an inhibitor of the MerTK receptor, a critical target in the regulation of tumor-associated macrophages (TAMs). This compound demonstrates the ability to effectively bind to MerTK in vivo, providing valuable insight into immune modulation in tumor microenvironments. MerTK-IN-1 is suitable for research applications focused on cancer immunotherapy and the role of macrophages in tumor progression. -
Gas6/Axl Inhibitor
Anticancer agent 109 is a Gas6/Axl inhibitor that demonstrates significant anti-cancer activity. This compound effectively downregulates the expression of Gas6 and Axl, which in turn reduces the activation of p-PI3K and p-AKT in cancer cells. Anticancer agent 109 induces G1 phase cell cycle arrest and promotes apoptosis, leading to substantial inhibition of tumor growth in nude mouse models. This reagent is suitable for research focused on cancer biology and therapeutic development targeting the Gas6/Axl signaling pathway. -
TYRO3/MERTK Inhibitor
UNC9435 is a dual inhibitor of TYRO3 and MERTK, exhibiting IC50 values of 3.7 nM and 1.1 nM, respectively. This compound has been shown to significantly reduce colony formation in non-small cell lung cancer cultures, indicating its potential as a therapeutic agent in cancer research. UNC9435 may also serve as a useful tool for studying the role of TYRO3 and MERTK in various biological processes and disease mechanisms. -
AXL Inhibitor
Axl-IN-3 is a selective inhibitor of the AXL kinase, demonstrating potent activity with an IC50 of 41.5 nM. This compound has shown minimal inhibition of other kinases, making it an ideal choice for studies focused on AXL-mediated signaling pathways. Axl-IN-3 is suitable for research applications involving cancer biology, immune modulation, and therapeutic resistance studies. -
MERTK/AXL Inhibitor
UNC8969 is a dual inhibitor targeting MERTK and AXL, exhibiting IC50 values of 1.1 ± 0.8 nM for MERTK and 5.3 ± 2.7 nM for AXL. With a half-life (T1/2) of 7.3 hours following intravenous administration at 5 mg/kg in mice, UNC8969 demonstrates significant biological activity. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating the roles of MERTK and AXL in tumor progression and immune modulation.
