2. Antibody-drug Conjugate/ADC Related Immunology/Inflammation Cell Cycle/DNA Damage
  3. Antibody-Drug Conjugates (ADCs) Transmembrane Glycoprotein Topoisomerase
  4. Precemtabart tocentecan

Precemtabart tocentecan  (Synonyms: Precem-TcT; M 9140)

目录号: HY-177434
产品使用指南 技术支持

Precemtabart tocentecan (Precem-TcT; M 9140) 是一种抗 CEACAM5 的抗体-药物偶联物 (ADC)。Precemtabart tocentecan 由肿瘤特异性的抗 CEACAM5 单克隆抗体 Precemtabart (HY-P990940)、一种高亲水性且稳定可切割的 β-葡萄糖醛酸苷连接子，以及 topoisomerase 1 抑制剂有效载荷 Exatecan (HY-13631) 组成，其用于 ADC 的药物-连接子偶联物为 Mal-Gly-PAB-Exatecan-D-glucuronic acid (HY-153179)。Precemtabart tocentecan 可抑制 CEACAM5 阳性癌细胞的生长。Precemtabart tocentecan 在表达 CEACAM5 的异种移植模型中表现出显著的抗肿瘤活性。Precemtabart tocentecan 可用于研究 CEACAM5 表达的晚期实体瘤。

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Precemtabart tocentecan

Precemtabart tocentecan Chemical Structure

CAS No. : 2873366-83-5

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Precemtabart tocentecan 相关抗体

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Topoisomerase Topo I Topo II

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Precemtabart tocentecan (Precem-TcT; M 9140) is an anti-CEACAM5 (carcinoembryonic antigen-related cell adhesion molecule 5) antibody-drug conjugate (ADC). Precemtabart tocentecan consists of a tumor-specific anti-CEACAM5 monoclonal antibody Precemtabart (HY-P990940), a highly hydrophilic and stable cleavable β-glucuronide linker, and a topoisomerase 1 inhibitor payload Exatecan (HY-13631), and the drug-linker conjugate for ADC is Mal-Gly-PAB-Exatecan-D-glucuronic acid (HY-153179). Precemtabart tocentecan inhibits the growth of CEACAM5-positive cancer cells. Precemtabart tocentecan exhibits significant antitumor activity in CEACAM5-expressing xenograft models. Precemtabart tocentecan can be used for the study of CEACAM5-expressing advanced solid tumors, especially mCRC[1].

IC50 & Target[1]

Topoisomerase I

 

体外研究
(In Vitro)

Precemtabart tocentecan (0.09-0.63 nM, 144 h) 可强效抑制 CEACAM5 阳性 SK-CO-1 和 MKN45 细胞的活力，其 IC50 值分别为 0.09 nM 和 0.63 nM[1].
Precemtabart tocentecan (1 nM, 6 days) 在与 CEACAM5 阳性 SK-CO-1 细胞共培养时，可诱导 CEACAM5 阴性 MDA-MB-231 细胞死亡，且随着 SK-CO-1 细胞数量的增加，该效应增强[1].

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

Precemtabart tocentecan 相关抗体:
体内研究
(In Vivo)

Precemtabart tocentecan (6 mg/kg, 静脉注射, 第 0 天给药一次) 在 CEACAM5 高表达的 COPF230 或 REPF210 癌来源异种移植模型中表现出显著的抗肿瘤活性[1].
Precemtabart tocentecan (4 mg/kg, 静脉注射, 每 2 周一次，共 3 次) 在 Irinotecan (HY-16562A) 预处理的 CXF4102 CRC PDX 模型中表现出显著的抗肿瘤活性[1].

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

Animal Model: COPF230 or REPF210 tumor fragments were subcutaneously implanted into the right flanks of 5-6-week-old female immunodeficient mice[1]
Dosage: 6 mg/kg
Administration: i.v., once on day 0
Result: Achieved tumor stasis (-29% tumor volume on day 52) in COPF230 model and tumor regression (-72% tumor volume on day 52) in REPF210 model.
Animal Model: CXF4102 tumor fragments were subcutaneously implanted into the right flanks of 6-8-week-old female immunodeficient mice[1]
Dosage: 4 mg/kg
Administration: i.v., once every 2 weeks for 3 doses
Result: Induced substantial tumor regression (-73% tumor volume on day 32) with sustained inhibition (-57% tumor volume on day 60) in irinotecan-pretreated CXF4102 model.
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
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

Precemtabart tocentecan 相关分类

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Keywords:

Precemtabart tocentecan2873366-83-5Precem-TcT M 9140M9140M 9140M-9140Antibody-Drug Conjugates (ADCs)Transmembrane GlycoproteinTopoisomeraseAntibody-Drug Conjugatesantibody-drug conjugateCEACAM5topoisomerase 1cancersInhibitorinhibitorinhibit

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