2. Metabolic Enzyme/Protease
  3. MMP
  4. 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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D8P1C1

D8P1C1 Chemical Structure

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D8P1C1 Related Antibodies

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Description

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[1][2][3].

Species Reactivity

Human
IC50 & Target[1]

ADAM17

180 pM (Kd)

In Vitro

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.

D8P1C1 Related Antibodies

ELISA Assay[1]

Cell Line: MDA-MB-231, HCC-827, OVCAR-3, Caov-3, COLO205
Concentration: 20 μg/mL
Incubation Time: 24 h
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%.

ELISA Assay[1]

Cell Line: MDA-MB-231, HCC-827, OVCAR-3, SKOV-3
Concentration: 10 μg/mL
Incubation Time: 4 h
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.
In Vivo

D8P1C1 (40 mg/kg; i.p.; bi-weekly; 4 weeks) achieves 25.4% tumor volume reduction in OVCAR-3 high-grade serous ovarian cancer xenografts in female NSG mice, with no observed toxicity[1].
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.

Animal Model: NSG mice (female, 6-8 weeks old, subcutaneously implanted with 10 × 106 OVCAR-3 cells)[1]
Dosage: 40 mg/kg
Administration: i.p.; bi-weekly; 4 weeks
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).
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]
Dosage: 15 mg/kg
Administration: i.p.; twice weekly; 4 weeks
Result: Achieved 78% tumor growth inhibition.
Showed no observable toxicity, with no mouse weight loss or visible diarrhea.
Gene ID

6868  [NCBI]

Accession
Target

ADAM17/TACE
Application

ELISA, FACS, Functional assay
Conjugated

Unconjugated
Reconsititution

The product can be reconstituted/diluted with sterile PBS or saline.
Formulation

Please refer to the lot-specific COA for specific buffer information.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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D8P1C1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

D8P1C1MMPMatrix metalloproteinasesADAM17high-grade serous ovarian cancercolon cancertriple-negative breast cancerovarian cancerlung adenocarcinomaMDA-MB-231gliomanon-high-grade serous ovarian cancerEGFRInhibitorinhibitorinhibit

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