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

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

Cat. No.: HY-177434
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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.

For research use only. We do not sell to patients.

Precemtabart tocentecan

Precemtabart tocentecan Chemical Structure

CAS No. : 2873366-83-5

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Description

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

 

In Vitro

Precemtabart tocentecan (0.09-0.63 nM, 144 h) potently inhibits the viability of CEACAM5-positive SK-CO-1 and MKN45 cells, with IC50 values of 0.09 nM and 0.63 nM respectively[1].
Precemtabart tocentecan (1 nM, 6 days) induces cell death in CEACAM5-negative MDA-MB-231 cells when co-cultured with CEACAM5-positive SK-CO-1 cells, and the effect is enhanced with increasing number of SK-CO-1 cells[1].

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

In Vivo

Precemtabart tocentecan (6 mg/kg, i.v., once on day 0) exerts potent antitumor activity, achieving tumor stasis in CEACAM5-high COPF230 or REPF210 cancer-derived xenograft model[1].
Precemtabart tocentecan (4 mg/kg, i.v., once every 2 weeks for 3 doses) exerts potent antitumor activity in Irinotecan (HY-16562A)-pretreated CXF4102 CRC PDX model[1].

MedChemExpress (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 No.
SMILES

[Precemtabart tocentecan]

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    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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