1. Antibody-drug Conjugate/ADC Related
  2. Antibody-Drug Conjugates (ADCs)
  3. Lupartumab Amadotin

Lupartumab Amadotin  (Synonyms: BAY 1129980; Anti-C4.4a antibody-drug conjugates)

Cat. No.: HY-P99719
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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.

Lupartumab Amadotin Chemical Structure

Lupartumab Amadotin Chemical Structure

CAS No. : 1640972-00-4

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Description

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[1].

IC50 & Target

human C4.4A[1]

In Vitro

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.

Cell Viability Assay[1]

Cell Line: hC4.4A:A549, mock:A549, NCI-H292, FaDu, NCI-H322, SCaBER and SCC-4 cells
Concentration: 0-2 nM
Incubation Time: 72 h
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.
In Vivo

Lupartumab Amadotin (BAY 1129980; 1.9-15 mg/kg; i.v.; Q4D×3) shows antitumor efficacy in the C4.4A-positive NCI-H292 and NCI-H322 NSCLC xenograft model[1].
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.

Animal Model: NMRI nu/nu mice, C4.4A-positive NCI-H292 human NSCLC xenograft model[1]
Dosage: 1.9, 3.75, 7.5 and 15 mg/kg
Administration: IV, Q4D×3
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.
CAS No.
SMILES

[Lupartumab Amadotin]

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Purity & Documentation
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  • 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.

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