Lupartumab Amadotin
Based on 1 Customer Validation
Lupartumab Amadotin (BAY 1129980) is an antibody–drug conjugate (ADC) consisting of a fully human C4.4A (LYPD3)-targeting mAb (BAY 1135626) (HY-147281) conjugated to a novel, highly potent derivative of the microtubule-disrupting cytotoxic drug auristatin via a noncleavable alkyl hydrazide linker. Lupartumab Amadotin can be used for the research of non-small cell lung cancer.
For research use only. We do not sell to patients.
- Purity: 99.61%
- CAS No.: 1640972-00-4
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Storage:
-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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
human C4.4A[1]
Lupartumab Amadotin (BAY 1129980; 0-2 nM; 72 h) demonstrates potent antiproliferative efficacy in cell lines endogenously expressing C4.4A and inhibits proliferation of C4.4A-transfected A549 lung cancer cells showing selectivity compared with a nontargeted control ADC[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:hC4.4A:A549, mock:A549, NCI-H292, FaDu, NCI-H322, SCaBER and SCC-4 cells
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Concentration:0-2 nM
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Incubation Time:72 h
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Result:High potency at subnanomolar range (IC50=0.05 nM) was observed in hC4.4A:A549 lung cancer cells, a remarkable selectivity (over 1,000-fold) compared with mock:A549 cells was observed. Showed high potency with IC50s at single- to double-digit nanomolar range and even at subnanomolar range (IC50 of 0.6 nM) in NCI-H292 lung cancer cell line.
Lupartumab Amadotin (BAY 1129980; 7.5 and 15 mg/kg; i.v.; Q4D×3) shows C4.4A target-dependent antitumor efficacy in NSCLC patient-derived xenograft (PDX) models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NMRI nu/nu mice, C4.4A-positive NCI-H292 human NSCLC xenograft model[1]
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Dosage:1.9, 3.75, 7.5 and 15 mg/kg
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Administration:IV, Q4D×3
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Result:Halted tumor growth dose dependently with a minimum effective dose (MED) of 1.9 mg/kg. The first treatment cycle with 15 mg/kg drug (Q4D×3) resulted in a marked delay of tumor growth with a significantly reduced tumor volume, as compared to vehicle, Cisplatin (HY-17394), or control ADC.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1640972-00-4
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Appearance Liquid
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Color Colorless to light yellow
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SMILES
[Lupartumab Amadotin]
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Synonyms
BAY 1129980; Anti-C4.4a antibody-drug conjugates
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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 (269 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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Lupartumab Amadotin Related Classifications
HY-P99719 Related Classifications
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