REGN5093-M114
Based on 1 Customer Validation
REGN5093-M114 is a biparatopic METxMET antibody-agent conjugate (ADC). REGN5093-M114 consists of the monoclonal anti-MET antibody Davutamig (HY-P990073) and a tubulin-inhibiting linker-payload (HY-148528). REGN5093-M114 binds distinct MET epitopes, inhibits MET recycling, and promotes lysosomal MET degradation, and its M114 payload inhibits Microtubule assembly and induces Apoptosis. REGN5093-M114 induces tumor regression in donor-derived xenograft models of EGFR-TKI-induced MET amplification and acquired MET alterations. REGN5093-M114 can be used for research on non-small cell lung cancer.
For research use only. We do not sell to patients.
- Antibody:
- Linker-Payload:
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Drug-to-Antibody Ratio:
3.2
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Conjugate Type:
Random Lysines
- Purity : 98.32%
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Storage:Shipping with dry ice
-80°C, protect from light
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[3]|
Met |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| EBC-1 | IC50 |
0.03 μg/mL
|
IC50 <0.03 μg/mL for inhibition of viability in EBC-1 NSCLC cells by CellTiter-Glo after 120 hrs.
IC50 <0.03 μg/mL for inhibition of viability in EBC-1 NSCLC cells by CellTiter-Glo after 120 hrs.
|
36269795 |
| NCI-H1993 | IC50 |
0.03 μg/mL
|
IC50 <0.03 μg/mL for inhibition of viability in H1993 NSCLC cells by CellTiter-Glo after 120 hrs.
IC50 <0.03 μg/mL for inhibition of viability in H1993 NSCLC cells by CellTiter-Glo after 120 hrs.
|
36269795 |
| HCC827 | IC50 |
0.22 μg/mL
|
IC50 0.22 μg/mL for inhibition of viability in HCC827 NSCLC cells by CellTiter-Glo after 120 hrs.
IC50 0.22 μg/mL for inhibition of viability in HCC827 NSCLC cells by CellTiter-Glo after 120 hrs.
|
36269795 |
| HCC4006 | IC50 |
0.27 μg/mL
|
IC50 0.27 μg/mL for inhibition of viability in H4006 NSCLC cells by CellTiter-Glo after 120 hrs.
IC50 0.27 μg/mL for inhibition of viability in H4006 NSCLC cells by CellTiter-Glo after 120 hrs.
|
36269795 |
| HCC4006 | IC50 |
3 μg/mL
|
IC50 >3 μg/mL for inhibition of viability in H4006-AR NSCLC cells by CellTiter-Glo after 120 hrs.
IC50 >3 μg/mL for inhibition of viability in H4006-AR NSCLC cells by CellTiter-Glo after 120 hrs.
|
36269795 |
| NCI-H522 | IC50 |
3 μg/mL
|
IC50 >3 μg/mL for inhibition of viability in H522 NSCLC cells by CellTiter-Glo after 120 hrs.
IC50 >3 μg/mL for inhibition of viability in H522 NSCLC cells by CellTiter-Glo after 120 hrs.
|
36269795 |
| NCI-H596 | IC50 |
3 μg/mL
|
IC50 >3 μg/mL for inhibition of viability in H596 NSCLC cells by CellTiter-Glo after 120 hrs.
IC50 >3 μg/mL for inhibition of viability in H596 NSCLC cells by CellTiter-Glo after 120 hrs.
|
36269795 |
| NCI-H460 | IC50 |
3 μg/mL
|
IC50 >3 μg/mL for inhibition of viability in H460 NSCLC cells by CellTiter-Glo after 120 hrs.
IC50 >3 μg/mL for inhibition of viability in H460 NSCLC cells by CellTiter-Glo after 120 hrs.
|
36269795 |
| H1975 | IC50 |
3 μg/mL
|
IC50 >3 μg/mL for inhibition of viability in H1975 NSCLC cells by CellTiter-Glo after 120 hrs.
IC50 >3 μg/mL for inhibition of viability in H1975 NSCLC cells by CellTiter-Glo after 120 hrs.
|
36269795 |
| NCI-H1650 | IC50 |
3 μg/mL
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IC50 >3 μg/mL for inhibition of viability in H1650 NSCLC cells by CellTiter-Glo after 120 hrs.
IC50 >3 μg/mL for inhibition of viability in H1650 NSCLC cells by CellTiter-Glo after 120 hrs.
|
36269795 |
| PC-9 | IC50 |
3 μg/mL
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IC50 >3 μg/mL for inhibition of viability in PC9 NSCLC cells by CellTiter-Glo after 120 hrs.
IC50 >3 μg/mL for inhibition of viability in PC9 NSCLC cells by CellTiter-Glo after 120 hrs.
|
36269795 |
| A549 | IC50 |
3 μg/mL
|
IC50 >3 μg/mL for inhibition of viability in A549 NSCLC cells by CellTiter-Glo after 120 hrs.
IC50 >3 μg/mL for inhibition of viability in A549 NSCLC cells by CellTiter-Glo after 120 hrs.
|
36269795 |
| NCI-H2291 | IC50 |
3 μg/mL
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IC50 >3 μg/mL for inhibition of viability in H2291 NSCLC cells by CellTiter-Glo after 120 hrs.
IC50 >3 μg/mL for inhibition of viability in H2291 NSCLC cells by CellTiter-Glo after 120 hrs.
|
36269795 |
In Vitro
REGN5093-M114 decreases viability in MET-overexpressing NSCLC cells, including cells without MET amplification, and its activity tracks MET surface expression rather than EGFR expression[1].
REGN5093-M114 response is predicted by MET surface expression ≥136.5 MFI and MET amplification CNV ≥2.5 in responder versus non-responder NSCLC cells, with combined expression/amplification status showing the highest predictive value[1].
REGN5093-M114 is active in organoids, primary cells, and ATCC cell lines, including TKI-naïve EGFR-mutant NSCLC cells with c-MET overexpression, irrespective of MET gene copy number[2].
REGN5093-M114 (0-3 μg/mL; 120 h) potently reduces viability of MET-amplified/overexpressed 2D NSCLC cells, including HCC827-AR (IC50 <0.03 μg/mL) and YU-1089 (IC50 0.05 μg/mL), while nonresponsive lines have IC50 >3 μg/mL[3].
REGN5093-M114 binding tracks cell-surface MET, with insensitive cells showing lower MET, although YUO-010 remains highly sensitive despite low surface MET[3].
REGN5093-M114 sensitivity is predicted by surface MET MFI ≥136.5, and combining MET expression with amplification yields AUC 1.0[3].
REGN5093-M114 (0.03-3 μg/mL; 5 days) retains single-agent antiproliferative activity but is not synergistic with Osimertinib (HY-15772) or Gefitinib (HY-50895) in HCC827-AR, YU-1089, YUO-010, YUO-006, YU-1095, and H820[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
REGN5093-M114 induces tumor regression in a MET Y1230C NSCLC PDX model and shows greatest efficacy among evaluated agents in PDX with acquired MET or other alterations[1].
REGN5093-M114 reduces tumor growth in EGFR-mutant NSCLC donor-derived models, including models with PTEN loss or c-MET-Y1230C mutation and prior osimertinib/savolitinib exposure[2].
REGN5093-M114 (10 mg/kg; s.c.; two doses separated by 1 week) produces pronounced tumor regression in YU-1089 EGFR-mutant NSCLC xenografts[3].
REGN5093-M114 (10 mg/kg) produces durable tumor regression in YHIM-1035 EGFR-mutant NSCLC PDX tumors[3].
REGN5093-M114 (10 mg/kg) produces durable tumor regression in YHIM-1042 EGFR-mutant NSCLC PDX tumors[3].
REGN5093-M114 (10 mg/kg) promotes tumor regression in YHIM-1061 EGFR-mutant NSCLC PDX tumors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:nu/nu (female, 6 weeks old)[3]
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Dosage:10 mg/kg
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Administration:s.c.; two doses separated by 1 week
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Result:Produced pronounced tumor regression, with tumor growth inhibition of 216.7%.
IHC showed marked reduction in p-MET, t-MET, and Ki67 staining.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Lysosome and acidic-vesicle live-cell staining
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Product Details
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Antibody
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Linker-Payload
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Drug-to-Antibody Ratio
3.2
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Conjugate Type
Random Lysines
Chemical Information
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Appearance Liquid
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Color Colorless to light yellow
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SMILES
[REGN5093-M114]
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Shipping
Shipping with dry ice.
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Storage
-80°C, protect from light
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Dardare J, et al. REGN5093-M114: can an antibody-drug conjugate overcome the challenge of resistance to epidermal growth factor receptor and mesenchymal epithelial transition tyrosine kinase inhibitors in non-small cell lung cancer? Transl Lung Cancer Res. 2024 Aug 31;13(8):2082-2086. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
REGN5093-M114 Related Classifications
HY-171191 Related Classifications
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