1. Antibody-drug Conjugate/ADC Related Cytoskeleton Cell Cycle/DNA Damage
  2. Antibody-Drug Conjugates (ADCs) Microtubule/Tubulin
  3. Cofetuzumab pelidotin

Cofetuzumab pelidotin  (Synonyms: PF-06647020; ABBV-647; h6M24-vc0101)

目录号: HY-P99829 纯度: 99.67%
COA

Cofetuzumab pelidotin (PF-06647020) 是一种靶向 PTK7ADC,包含人源化抗 PTK7 mAb (hu6M024;IgG1),通过可裂解的缬氨酸-瓜氨酸 (vc) 的 linker 与 auristatin 微管抑制剂 Auristatin-0101 (Aur0101;HY-12522) 连接。Cofetuzumab pelidotin 的 DAR 为 4。Cofetuzumab pelidotin 与细胞表面 PTK7 结合的 EC50 为 1153 pM (通过流式细胞术检测)。Cofetuzumab pelidotin 具有用于实体瘤研究的潜力。

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Cofetuzumab pelidotin Chemical Structure

Cofetuzumab pelidotin Chemical Structure

CAS No. : 1869937-48-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cofetuzumab pelidotin (PF-06647020) is a PTK7-targeting ADC comprising a humanized anti-PTK7 mAb (hu6M024, IgG1) joined to an auristatin microtubule inhibitor payload, auristatin-0101 (Aur0101; HY-12522), by a cleavable valine-citrulline (vc)-based linker. Cofetuzumab pelidotin has a DAR of 4. Cofetuzumab pelidotin binds to cell-surface PTK7 with an EC50 of 1153 pM by flow cytometry. Cofetuzumab pelidotin has the potential for solid tumors research[1][2][3].

体外研究
(In Vitro)

Cofetuzumab pelidotin (PF-06647020) 对表达 PTK7 的癌细胞系 H446、H661 和 OVCAR3 具有体外细胞毒性作用,EC50 值分别为 7.6、27.5 和 105 ng/mL[1]
Cofetuzumab pelidotin (持续 6 天)在一组癌细胞系 (A549、MDA-MB-468、KYSE-150、SKOV-3、PC9、NCI-H1975) 细胞中显示出高效力和 PTK7 特异性细胞毒性,IC50 为 0-1100 nM[2]
Cofetuzumab pelidotin 稳定性较差,T1/2 不足 3 天[2]

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

体内研究
(In Vivo)

Cofetuzumab pelidotin (PF-06647020;3 mg/kg;腹腔注射,每周两次,持续四个周期) 对 NSCLC、OVCA 和 TNBC 的 PDX 小鼠模型产生显着抗肿瘤作用[1]

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

Animal Model: 6- to 10-week-old NOD scid mice with NSCLC, OVCA and TNBC cells[1]
Dosage: 3 mg/kg
Administration: Intraperitoneal injection twice a week for four cycles
Result: Induced striking in vivo anti-tumor effects on a subset of patient–derived xenografts (PDXs) derived from NSCLC, OVCA and TNBC.
CAS 号
性状

液体

颜色

Colorless to light yellow

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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Cofetuzumab pelidotin
目录号:
HY-P99829
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