D8P1C1
D8P1C1 is a high-affinity ADAM17 inhibitor (with a Kd of 180 pM targeting ADAM17-ECD) that reduces the shedding and phosphorylation of EGFR ligands. D8P1C1 inhibits cancer cell proliferation in vitro and tumor growth in xenograft models. 89Zr-DFO-D8P1C1 radioimmunological PET imaging shows its substantial accumulation in ovarian tumor xenografts, serving as a platform for generating bispecific T-cell engager derivatives. D8P1C1 can be applied to research on related diseases including triple-negative breast cancer, various types of ovarian cancer, lung adenocarcinoma, glioma, and colon cancer.
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Activité biologique
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Chemical Information
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Help & FAQs
Activité biologique
Human
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ADAM17 180 pM (Kd) |
D8P1C1 (20 μg/mL; 24 h) potently inhibits shedding of EGFR ligands, TNFα, and CX3CL1, but only weakly inhibits Notch1 cleavage, in MDA-MB-231, HCC-827, OVCAR-3, Caov-3, and COLO205 cells[1].
D8P1C1 (10 μg/mL; 4 h) potently inhibits EGFR phosphorylation in MDA-MB-231, HCC-827, OVCAR-3, and SKOV-3 cells[1].
D8P1C1 (0.037 µg/mL; 38 h) inhibits proliferation of triple-negative breast cancer MDA-MB-231 cells with an IC50 of 0.037 µg/mL[2].
D8P1C1 (0.625-20 µg/mL; 38 h) inhibits proliferation of SKBR-3, HCC-827, LIM1215, U-87 MG, SKOV-3, OVCAR-3, and CAOV-3 cancer cells, with the greatest efficacy observed in HER2-overexpressing breast SKBR-3 cells[2].
D8P1C1 (7.8125-250 µM; 2 h) preferentially binds to ADAM17 expressed on MDA-MB-231, SKBR-3, HCC-827, LIM1215, U-87 MG, OVCAR-3, SKOV-3, and CAOV-3 cancer cells, with binding affinity approximately 6-fold higher than for ADAM17 on HEK293 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, HCC-827, OVCAR-3, Caov-3, COLO205
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Concentration:20 μg/mL
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Incubation Time:24 h
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Result:Inhibited shedding of EGFR ligands (EGF, TGFα, AREG) with 78-87% efficiency across all tested cell lines.
Inhibited TNFα shedding by 78%, CX3CL1 shedding by 70%, and Notch1 cleavage (measured as NICD1 release) by 15%.
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Cell Line:MDA-MB-231, HCC-827, OVCAR-3, SKOV-3
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Concentration:10 μg/mL
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Incubation Time:4 h
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Result:Inhibited EGFR phosphorylation by 95% in MDA-MB-231 cells, 91% in HCC-827 cells, 87% in OVCAR-3 cells, and 71% in SKOV-3 cells.
Showed no significant change in total EGFR levels in most cell lines.
D8P1C1 (60 mg/kg) achieves 45% tumor growth inhibition in SKOV-3 non-high-grade serous ovarian cancer xenografts in NSG mice, with no observed toxicity[1].
D8P1C1 (15 mg/kg; i.p.; twice weekly; 4 weeks) achieves 78% tumor growth inhibition in a mouse TNBC xenograft model, with no observable toxicity[2].
D8P1C1 (60 mg/kg; i.p.; twice weekly; 4 weeks) achieves 45% tumor growth inhibition in a mouse ovarian cancer xenograft model, with no observable toxicity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice (female, 6-8 weeks old, subcutaneously implanted with 10 × 106 OVCAR-3 cells)[1]
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Dosage:40 mg/kg
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Administration:i.p.; bi-weekly; 4 weeks
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Result:Decreased average tumor volume by 25.4% on day 47 after tumor cell implantation.
Showed no discernible toxicity (e.g., no diarrhea or decrease in body weight).
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Animal Model:Athymic nude mice (6- to 8-week-old female; triple-negative breast cancer xenograft via subcutaneous implantation of 10 million MDA-MB-231 cells)[2]
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Dosage:15 mg/kg
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Administration:i.p.; twice weekly; 4 weeks
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Result:Achieved 78% tumor growth inhibition.
Showed no observable toxicity, with no mouse weight loss or visible diarrhea.
ADAM17/TACE
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Product Image
ELISA, FACS, Functional assay
Chemical Information
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Saha N, et al. Characterization of the D8P1C1 Anti-ADAM17 Inhibitory Monoclonal Antibody and Generation of Its Bispecific T-Cell Engager Derivative. Int J Mol Sci. 2026;27(7):2936. Published 2026 Mar 24. [Content Brief]
[2]. Saha N, et al. Inhibitory monoclonal antibody targeting ADAM17 expressed on cancer cells. Transl Oncol. 2022;15(1):101265. [Content Brief]
[3]. Arora S, et al. ADAM Proteases in Cancer: Biological Roles, Therapeutic Challenges, and Emerging Opportunities. Cancers (Basel). 2025;17(10):1703. Published 2025 May 19. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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