c-Met/HGFR Inhibitor

VEGFR-2/c-Met-IN-2 (compound 3e) is a VEGFR-2/c-Met inhibitor, with IC₅₀ values of 83 and 48 nM, respectively. VEGFR-2/c-Met-IN-2 exhibits cytotoxic activity against HCT-116 cell line (IC₅₀: 3.403 µM).

c-Met-IN-18 is ATP competitive type-III c-MET inhibitor of WT and D1228V mutant c-MET. c-Met-IN-18 has inhibitory for WT/D1228V with an IC₅₀ value of 0.013/0.20^e.c-Met-IN-18 can be used for the research of c-MET driven cancers. c-Met-IN-18 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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.

c-Met/HDAC-IN-3 (Compound 15f) is a dual c-Met and HDAC inhibitor with IC₅₀ values of 12.50 nM and 26.97 nM against c-Met and HDAC1, respectively. c-Met/HDAC-IN-3 induces apoptosis and cause cell cycle arrest in G2/M phase.

Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.

PF 04254644 is an orally active c-Met inhibitor. PF 04254644 inhibits mesenchymal transfer factor/hepatocyte growth factor receptor. PF 04254644 induces myocardial degeneration in rats. PF 04254644 may be used in research on cardiovascular disease and cancer.

Anti-MSPR/RON/CD136 Antibody (H5B14) is a humanized antibody expressed in CHO cells, targeting MSPR/RON/CD136. Anti-MSPR/RON/CD136 Antibody (H5B14) has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 156.7 kDa. The isotype control for Anti-MSPR/RON/CD136 Antibody (H5B14) can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).

Mer/c-Met-IN-1 is a potent Mer/c-met dual inhibitor with IC₅₀ values of 1 and 19 nM. Mer/c-Met-IN-1 can inhibit cancer cells proliferation, migration and induce apoptosis. Mer/c-Met-IN-1 can be used for the research of cancer, such as colon cancer.

(R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) is an orally active, potent and irreversible dual specificity inhibitor of?ErbB?family (EGFR?and?HER2), with?IC₅₀?values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for?EGFR^wt, EGFR^L858R,?EGFR^L858R/T790M?and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung?cancer?(NSCLC) and gastric?cancer.

NSC 850745 is a selective and potent c-Met/STAT3 inhibitor with IC₅₀ values of 210 and 670 nM. NSC 850745 can inhibit cell proliferation, induce G2/M phase arrest and induce apoptosis. NSC 850745 can downregulate AKT-1, VEGF and Bcl-2 expression and upregulate p53, Bax and caspase expression. NSC 850745 can be used for the research of cancer, such as leukemia and colon cancer.

Telisotuzumab (ABT-700) (powder) is a bivalent humanized IgG1 anti-c-Met monoclonal antibody. Telisotuzumab (powder) binds cellular c-Met and disrupts its productive dimerization and activation induced by HGF or by the high density of c-Met on the cell surface independent of ligand. Telisotuzumab (powder) induces apoptosis. Telisotuzumab (powder) can be used for the study of cancers harboring amplified MET, such as gastric and lung cancers.

c-Met-IN-29 is an orally active c-Met inhibitor with an IC₅₀ of 1.6 nM. c-Met-IN-29 binds to and functionally modulates c-Met protein, inhibiting tumor cell proliferation, migration and apoptosis. c-Met-IN-29 exhibits anti-tumor activity both in vitro and in vivo. c-Met-IN-29 can be used for the research of non-small cell lung cancer.

Antitumor agent-45 (Compound 21) could induce and stimulate A549 cells apoptosis in G0/G1 and G2/M phase. Antitumor agent-45 (Compound 21) inhibits c-Met expression to regulate the growth of tumor cells.

c-Met/HDAC-IN-2 is a highly potent c-Met and HDAC dual inhibitor with IC₅₀s of 18.49 nM and 5.40 nM for HDAC1 and c-Met, respectively. c-Met/HDAC-IN-2 has antiproliferative activities against certain cancer cell lines. c-Met/HDAC-IN-2 can cause G2/M-phase arrest and induce apoptosis in HCT-116. c-Met/HDAC-IN-2 can be used for researching anti-cancer resistance.

Multi-kinase-IN-5 (compound 15c) is a promising multi-kinase inhibitory agent. Multi-kinase-IN-5 inhibits a panel of protein kinases (RET, KIT, cMet, VEGFR1,2, FGFR1, PDGFR and BRAF), showing % inhibition of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%, respectively, and IC₅₀ of 1.287, 0.117 and 1.185 μM against FGFR1, VEGFR, and RET kinases, respectively.

Zgwatinib (SOMG-833) is a potent, selective, and ATP-competitive c-MET inhibitor, with an IC₅₀ of 0.93 nM against c-MET, over 10,000-fold more potent compared with 19 tyrosine kinases (including c-MET family members and highly homologous kinases). Zgwatinib potently inhibits c-MET-driven cell proliferation. Zgwatinib as a potential candidate agent for c-MET-driven human cancers research.

BMS-748730 is an oral tyrosine kinase inhibitor. BMS-748730 inhibits tyrosine kinase activity by competing with the ATP binding site of the tyrosine kinase, which prevents the kinase from phosphorylating the substrate protein, thereby inhibiting signaling pathways associated with cell proliferation and tumor growth. BMS-748730 can be used in the study of certain types of cancer, including chronic myeloid leukemia (CML).

SAIT-301 is a Met-targeting monoclonal antibody. SAIT-301 inhibits Met activation, induces downregulated expression of phosphorylated Met(p-Met) and phosphorylated ERK(p-ERK), and reduces EGR-1 expression. SAIT-301 inhibits the migration and invasion of nasopharyngeal carcinoma cells. SAIT-301 is applicable to relevant research on nasopharyngeal carcinoma. For the isotype control of SAIT-301, refer to Human IgG1 kappa, Isotype Control (HY-P99001).

VEGFR-2-IN-89 is a VEGFR-2 inhibitor with an IC₅₀ of 77 nM. VEGFR-2-IN-89 potently inhibits c-Met kinase activity with an IC₅₀ of 0.152 μM, and also exhibits good inhibitory activity against EGFR (IC₅₀ = 0.269 μM) and PDGFR-β kinase (IC₅₀ = 0.301 μM). VEGFR-2-IN-89 displays anticancer activity against liver cancer. VEGFR-2-IN-89 can be used in the research of hepatocellular carcinoma.

c-Met-IN-23 (Compound 12g) is a c-Met inhibitor (IC₅₀ = 0.052 μM for c-Met). c-Met-IN-23 also inhibits MDR1 and MRP1/2 pumps in the cancerous HepG2 and BxPC3 cells. c-Met-IN-23 is an anticancer agent.