Precemtabart tocentecan
Based on 1 Customer Validation
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.
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- Pureté: 99.31%
- CAS No.: 2873366-83-5
- Masse moléculaire:152832 (average)
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Stockage:
-80°C, protect from light
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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Topoisomerase I |
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.
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.
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Animal Model:COPF230 or REPF210 tumor fragments were subcutaneously implanted into the right flanks of 5-6-week-old female immunodeficient mice[1]
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Dosage:6 mg/kg
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Administration:i.v., once on day 0
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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.
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Animal Model:CXF4102 tumor fragments were subcutaneously implanted into the right flanks of 6-8-week-old female immunodeficient mice[1]
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Dosage:4 mg/kg
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Administration:i.v., once every 2 weeks for 3 doses
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2873366-83-5
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Appearance Liquid
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Masse moléculaire 152832 (average)
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Color Colorless to light yellow
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SMILES
[Precemtabart tocentecan]
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Synonyms
Precem-TcT; M 9140
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Livraison
Shipping with dry ice.
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Stockage
-80°C, protect from light
Pureté et documentation
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Fiche technique (268 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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