KTN0073
KTN0073 is a high-affinity MET receptor tyrosine kinase inhibitor. KTN0073 can be used in studies related to non-small cell lung cancer and human cancers driven by HGF, MET amplification, or exon 14 mutation. KTN0073 binds to the Sema/PSI domain to block the HGF-MET interaction, and induces ubiquitination and degradation of oncogenic MET receptors via an HGF-independent pathway, thereby inhibiting MET-dependent signal transduction. KTN0073 exhibits significant antitumor activity in vivo, and its tumor suppressive activity is superior to that of the IgG1 subtype when grafted to the IgG2 constant region.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Human IgG2 kappa
Human
KTN0073 (Serial dilutions; 2 hours) potently inhibits HGF-stimulated MET phosphorylation in A549 cells with an IC50 ranging from 40 to 217 pmol/L[2].
KTN0073 (Up to 100 nmol/L; 4 to 5 days) inhibits HGF-induced U87MG cell spheroid proliferation without exhibiting agonistic activity[2].
KTN0073 (1 nmol/L; 2 hours) inhibits HGF-stimulated phosphorylation of MET, Akt, and MAPK in A549 cells to levels comparable to crizotinib[2].
KTN0073 (1 nmol/L; 15 minutes) induces potent ubiquitination of MET in A549 cells after 15 minutes[2].
KTN0073 (1 nmol/L; 24 hours) does not induce MET shedding in A549 cells after 24 hours, unlike PMA treatment[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87MG cells
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Concentration:Up to 100 nmol/L
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Incubation Time:4 to 5 days (with HGF)
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Result:Inhibited HGF-induced U87MG spheroid proliferation with no agonistic activity observed in the absence of exogenous HGF.
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Cell Line:A549 cells
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Concentration:1 nmol/L
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Incubation Time:2 hours (preincubated prior to 10-minute HGF stimulation)
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Result:Inhibited HGF-induced phosphorylation of MET, Akt, and MAPK to levels comparable to the MET kinase inhibitor crizotinib.
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Cell Line:SNU5 cells (MET-amplified), EBC1 cells (MET-amplified)
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Concentration:Serial dilutions
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Incubation Time:5 days
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Result:Induced 86% and 97% inhibition of cell proliferation in SNU5 and EBC1 cells, respectively, whereas KTN0073-IgG1 and KTN0073-IgG4 showed no inhibition.
KTN0073 (3 mg/kg; i.p.; 2 doses on days 0 and 3) induces significant MET protein degradation in U87MG glioma xenografts, reducing MET-positive staining to 6.7%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (female, 6 to 8 weeks old, subcutaneous xenograft with human U87MG glioma cells)[2]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:i.p.; biweekly
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Result:Induced potent growth inhibition of established U87MG tumors.
Resulted in tumor growth inhibition comparable to 50 mg/kg crizotinib at 30 mg/kg.
Was well-tolerated with no weight loss or observational toxicity reported.
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Animal Model:BALB/c nude mice (female, 6 to 8 weeks old, subcutaneous xenograft with human U87MG glioma cells)[2]
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Dosage:3 mg/kg
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Administration:i.p.; 2 doses on days 0 and 3
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Result:Reduced MET-positive staining to 6.7% in treated tumors, compared to 37.4% for PBS-treated tumors and 34.6% for control antibody-treated tumors.
HGFR/c-Met
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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ELISA, FACS, Functional assay
Chemical Information
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Stella GM, et al. Brain Metastases from Lung Cancer: Is MET an Actionable Target?. Cancers (Basel). 2019;11(3):271. Published 2019 Feb 26. [Content Brief]
[2]. Yang Y, et al. Antitumor Properties of an IgG2-Enhanced Next-Generation MET Monoclonal Antibody That Degrades Wild-Type and Mutant MET Receptors. Cancer Res. 2016;76(19):5788-5797. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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