DT-9081
DT-9081 is an orally active and selective EP4 receptor antagonist, IC50 = 2.49 nM. DT-9081 blocks PGE2/EP4R-mediated cAMP signaling, counteracts EP4R-driven immunosuppression, and restores antitumor immunity. DT-9081 combined with anti-PD-1 antibody significantly improves tumor growth inhibition and animal survival in mouse tumor models. DT-9081 can be used in cancer-related research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2639645-80-8
- Formel: C25H29F3N2O4
- Molecular Weight:478.50
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
EP4 2.49 nM (IC50) |
CYP2C8 11.7 μM (IC50) |
CYP2C19 3.17 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
2.49 nM
|
Antagonism of human EP4 receptor in HEK-293 cells assessed by EPAC BRET cAMP assay with Prolume Purple luciferase substrate and 20 min BRET recording after EC80 TCS2510 stimulation.
Antagonism of human EP4 receptor in HEK-293 cells assessed by EPAC BRET cAMP assay with Prolume Purple luciferase substrate and 20 min BRET recording after EC80 TCS2510 stimulation.
|
acs.jmedchem.6c00863 |
| HEK293 | IC50 |
3.68 nM
|
Antagonism of mouse EP4 receptor in HEK-293 cells assessed by EPAC BRET cAMP assay with Prolume Purple luciferase substrate and 20 min BRET recording after EC80 TCS2510 stimulation.
Antagonism of mouse EP4 receptor in HEK-293 cells assessed by EPAC BRET cAMP assay with Prolume Purple luciferase substrate and 20 min BRET recording after EC80 TCS2510 stimulation.
|
acs.jmedchem.6c00863 |
| HEK293 | IC50 |
7.00 nM
|
Antagonism of rat EP4 receptor in HEK-293 cells assessed by EPAC BRET cAMP assay with Prolume Purple luciferase substrate and 20 min BRET recording after EC80 TCS2510 stimulation.
Antagonism of rat EP4 receptor in HEK-293 cells assessed by EPAC BRET cAMP assay with Prolume Purple luciferase substrate and 20 min BRET recording after EC80 TCS2510 stimulation.
|
acs.jmedchem.6c00863 |
| HEK293 | IC50 |
21.46 nM
|
Antagonism of dog EP4 receptor in HEK-293 cells assessed by EPAC BRET cAMP assay with Prolume Purple luciferase substrate and 20 min BRET recording after EC80 TCS2510 stimulation.
Antagonism of dog EP4 receptor in HEK-293 cells assessed by EPAC BRET cAMP assay with Prolume Purple luciferase substrate and 20 min BRET recording after EC80 TCS2510 stimulation.
|
acs.jmedchem.6c00863 |
In Vitro
DT-9081 (compound 10m) is a potent antagonist of human EP4R in the human HEK-293 EPAC BRET cAMP assay, with an IC50 of 2.49 nM, and maintains nanomolar potency against mouse, rat, and dog EP4R; it blocks EP4R/cAMP signaling in human IL-2-activated T cells, with an IC50 of 65 nM[1].
DT-9081 binds EP4R with an inhibition rate of 100.1% and is highly selective for other prostanoid receptors[1].
DT-9081 (10 μM) shows no significant off-target activity in the Safety Screen 87 panel, except for 62% binding inhibition of 5-HT2B, and has no functional 5-HT2B activity[1].
DT-9081 exhibits acceptable cross-species in vitro stability, a high plasma protein binding rate, and inhibits CYP2C8/2C19 and OATP1B1/1B3/BCRP[1].
DT-9081 (30 μM) weakly inhibits hERG in stably transfected CHO cells, with an inhibition rate of 16.7%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | CL | Vdss | T1/2 | Tmax | Cmax | AUClast | F |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 0.2 L/h/kg | 0.4 L/kg | 1.5 h | / | / | / | / |
| Mice[1] | 30 mg/kg | p.o. | / | / | / | 0.4 h | 19032 ng/mL | 65375 ng·h/mL | 44 % |
| Mice[1] | 10 mg/kg | p.o. | / | / | / | / | 4591 ng/mL | 25204 ng·h/mL | 51 % |
| Rat[1] | 2 mg/kg | i.v. | 0.05 L/h/kg | 0.4 L/kg | 4.7 h | / | / | / | / |
| Rat[1] | 10 mg/kg | p.o. | / | / | / | 4.0 h | 11897 ng/mL | 158721 ng·h/mL | 85 % |
| Dog[1] | 1 mg/kg | i.v. | 0.005 L/h/kg | 0.12 L/kg | 16.5 h | / | / | / | / |
| Dog[1] | 3 mg/kg | p.o. | / | / | / | 0.5 h | 23016 ng/mL | 287261 ng·h/mL | 74 % |
In Vivo
DT-9081 (30 mg/kg; p.o.; twice daily; day 8 to day 28) shows low single-agent activity in the 4T1 triple-negative breast cancer model, but when combined with anti-PD-1 and Cisplatin (HY-17394), it increases the response rate[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2639645-80-8
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Molecular Weight 478.50
-
Formel C25H29F3N2O4
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SMILES
O=C(O)C1=CC=C([C@@H](NC(CC(C)(N2C[C@H](OC3=CC=CC(C(F)(F)F)=C3)CC2)C)=O)C)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Research Protocol for Cancer Immunology
Cancer immunology studies how the immune system recognizes, suppresses, edits, or fails to eliminate malignant cells through tumor antigen release, antigen presentation, T-cell priming, immune trafficking, tumor-cell killing, and feedback inhibition in the tumor microenvironment. The cancer-immunity cycle links tumor antigenicity, dendritic-cell priming, CD8+ T-cell infiltration, cytotoxic function, and immune-checkpoint regulation to tumor rejection or immune escape. Immune-checkpoint pathways such as PD-1/PD-L1 and CTLA-4 suppress antitumor T-cell activity and can be therapeutically blocked, but many tumors remain resistant because of poor antigen presentation, weak T-cell infiltration, suppressive myeloid cells, regulatory T cells, and tumor-intrinsic immune-exclusion programs. Unresolved questions include which immune-cell states predict response, how tumor-intrinsic pathways exclude immune cells, how myeloid suppression limits checkpoint blockade, and which combination strategies
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)