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)

目录号: HY-P99719 纯度: 99.61%
COA 产品使用指南 技术支持

Lupartumab Amadotin (BAY 1129980) 是一种由全人源 C4.4A (LYPD3) 靶向单抗 (BAY 1135626) (HY-147281) 通过不可切割的烷基肼连接物与一种新型、高效的微管破坏细胞毒药物 auristatin 衍生物结合的抗体-药物偶联物 (ADC)。Lupartumab Amadotin 可用于非小细胞肺癌的研究。

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Lupartumab Amadotin

Lupartumab Amadotin Chemical Structure

CAS No. : 1640972-00-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]

体外研究
(In Vitro)

Lupartumab Amadotin (BAY 1129980; 0-2 nM; 72 h) 在内源性表达 C4.4A 的细胞系中显示出强大的抗增殖功效,并抑制 C4.4A 转染的 A549 肺癌细胞的增殖,与非靶向对照 ADC 相比显示出选择性[1]

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.
体内研究
(In Vivo)

Lupartumab Amadotin (BAY 1129980; 1.9-15 mg/kg; i.v.; Q4D×3) 在 C4.4A 阳性的 NCI-H292 和 NCI-H322 NSCLC 异种移植模型中显示出抗肿瘤效果[1]
Lupartumab Amadotin (BAY 1129980; 7.5 and 15 mg/kg; i.v.; Q4D×3) 显示在 NSCLC 患者源性异种移植 (PDX) 模型中 C4.4A 靶点依赖的抗肿瘤疗效[1]

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 号
性状

液体

颜色

Colorless to light yellow

中文名称

阿汀-鲁帕妥单抗

运输条件

Shipping with dry ice.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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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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Lupartumab Amadotin
目录号:
HY-P99719
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