2. Antibody-drug Conjugate/ADC Related Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. EGFR Antibody-Drug Conjugates (ADCs)
  4. Depatuxizumab mafodotin

Depatuxizumab mafodotin  (Synonyms: ABT-414)

目录号: HY-132259 纯度: 99.73%
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Depatuxizumab mafodotin (ABT-414) 是一种抗体-药物偶联物 (ADC)，能够特异性地靶向表皮生长因子受体 (EGFR)。Depatuxizumab mafodotin 可以用于胶质瘤、头颈部鳞状细胞癌、非小细胞肺癌、皮肤表皮样癌、舌鳞状细胞癌的研究。

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Depatuxizumab mafodotin Chemical Structure

Depatuxizumab mafodotin Chemical Structure

CAS No. : 1585973-65-4

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Depatuxizumab mafodotin 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Depatuxizumab mafodotin (ABT-414) is an antibody-drug conjugate (ADC). Depatuxizumab mafodotin specifically targets the epidermal growth factor receptor (EGFR). Depatuxizumab mafodotin can be used in the study of glioma, head and neck squamous cell carcinoma, non-small cell lung cancer, epidermoid carcinoma of the skin, and squamous cell carcinoma of the tongue[1][2][3][4][5].

体外研究
(In Vitro)

Depatuxizumab mafodotin (最多 10 nM；最多 72 h) 可诱导过表达 EGFR 或 EGFRvIII 的胶质瘤细胞系细胞死亡[2]。
Depatuxizumab mafodotin (0-3.38 nM； 72 h) 以剂量依赖性方式诱导 EGFR 高表达的人头颈部鳞状细胞癌 (HNSCC) 细胞系 (UMSCC47 和 FaDu) 细胞死亡，对 UMSCC47 和 FaDu 细胞系的 IC50 值分别为 0.213 nM 和 0.167 nM[3]。
Depatuxizumab mafodotin 对过表达野生型或突变型 EGFR 的肿瘤细胞系表现出显著的细胞毒性[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Depatuxizumab mafodotin 相关抗体:
体内研究
(In Vivo)

Depatuxizumab mafodotin (8 mg/kg；腹腔注射；每 4 天一次；共 6 次) 导致免疫缺陷 CD1 裸鼠 LN-229 EGFRvIII 细胞原位移植模型中的肿瘤 EGFRvIII 表达丧失[2]。
Depatuxizumab mafodotin (4 mg/kg；腹腔注射；每 4 天一次；共 4 次) 显著抑制移植 FaDu 细胞系的雌性裸鼠的肿瘤生长[3]。
Depatuxizumab mafodotin (1-10 mg/kg；每 4 天一次；共 6 次) 显著延缓或抑制携带多种人类肿瘤异种移植瘤 (例如 A431、NCI-H1703、HCC827.ER.LMC、SCC-15) 小鼠，并可在某些模型中引起肿瘤消退甚至治愈[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Immunocompromised CD1 nude mice with LN-229 EGFRvIII cell orthotopic xenograft model[2]
Dosage: 8 mg/kg
Administration: Intraperitoneal administration, every 4 days, for a total of six doses
Result: Specifically and profoundly prolonged the survival of mice carrying EGFRvIII-expressing tumors.
Caused the loss of EGFRvIII expression in tumors.
Still caused loss of EGFRvIII several weeks after treatment ends.
Animal Model: Female SCID, SCID-Beige, and nude mice (weight: 20-22 g upon arrival, 6-8-week-old when tumor cells were implanted), U87MGde2-7 glioblastoma multiforme model, SN0199 and SN0207 glioblastoma multiforme patient-derived xenograft models. A431, NCI-H1703, HCC827.ER.LMC, SCC-15, LoVo, NCI-H441, SW48, A549, HCT-15 xenograft models[4]
Dosage: 0.5, 1, 2, 3, 4, 10 mg/kg
Administration: once every 4 days, a total of 6 administrations
Result: Led to complete tumor regression and cure in the U87MGde2-7 glioblastoma model.
Caused significant tumor growth inhibition and regression in the SN0199 and SN0207 glioblastoma multiforme patient-derived xenograft models.
Did not show significant effects in some models like A549 and HCT-15 with lower levels of EGFR.
Clinical Trial
CAS 号
性状

液体

颜色

Colorless to light yellow

运输条件

Shipping with dry ice.
储存方式

-80°C, protect from light
纯度 & 产品资料
参考文献

Depatuxizumab mafodotin 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Depatuxizumab mafodotin1585973-65-4ABT-414ABT414ABT 414EGFRAntibody-Drug Conjugates (ADCs)Epidermal growth factor receptorErbB-1HER1Antibody-Drug ConjugatesCancerEpidermal growth factor receptor (EGFR)A431NCI-H1703HCC827.ER.LMCSCC-15LoVoNCI-H441SW48A549HCT-15Inhibitorinhibitorinhibit

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