2. Protein Tyrosine Kinase/RTK
  3. c-Met/HGFR
  4. 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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KTN0073

KTN0073 Chemical Structure

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KTN0073 Related Antibodies

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Description

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[1][2].

Isotype

Human IgG2 kappa
Recommend Isotype Controls
Species Reactivity

Human
In Vitro

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.

KTN0073 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: U87MG cells
Concentration: Up to 100 nmol/L
Incubation Time: 4 to 5 days (with HGF)
Result: Inhibited HGF-induced U87MG spheroid proliferation with no agonistic activity observed in the absence of exogenous HGF.

Western Blot Analysis[2]

Cell Line: A549 cells
Concentration: 1 nmol/L
Incubation Time: 2 hours (preincubated prior to 10-minute HGF stimulation)
Result: Inhibited HGF-induced phosphorylation of MET, Akt, and MAPK to levels comparable to the MET kinase inhibitor crizotinib.

Cell Proliferation Assay[2]

Cell Line: SNU5 cells (MET-amplified), EBC1 cells (MET-amplified)
Concentration: Serial dilutions
Incubation Time: 5 days
Result: Induced 86% and 97% inhibition of cell proliferation in SNU5 and EBC1 cells, respectively, whereas KTN0073-IgG1 and KTN0073-IgG4 showed no inhibition.
In Vivo

KTN0073 (1-30 mg/kg; i.p.; biweekly) potently inhibits growth of U87MG glioma xenografts at doses as low as 1 mg/kg, with 30 mg/kg activity matching that of 50 mg/kg crizotinib[2].
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.

Animal Model: BALB/c nude mice (female, 6 to 8 weeks old, subcutaneous xenograft with human U87MG glioma cells)[2]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: i.p.; biweekly
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.
Animal Model: BALB/c nude mice (female, 6 to 8 weeks old, subcutaneous xenograft with human U87MG glioma cells)[2]
Dosage: 3 mg/kg
Administration: i.p.; 2 doses on days 0 and 3
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.
Gene ID

4233  [NCBI]

Accession
Target

HGFR/c-Met
Application

ELISA, FACS, Functional assay
Conjugated

Unconjugated
Reconsititution

The product can be reconstituted/diluted with sterile PBS or saline.
Formulation

Please refer to the lot-specific COA for specific buffer information.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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KTN0073 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KTN0073KTN 0073KTN-0073c-Met/HGFRnon-small cell lung cancerMET-amplified cellsA549 cellsHGF-MET interactionU87MG cellsSema/PSI domainMET receptor tyrosine kinaseH596 cellsDU145 cellsMET juxtamembrane exon 14 deletion mutantsInhibitorinhibitorinhibit

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