DT-9081 hydrochloride
DT-9081 hydrochloride is an orally active and selective EP4 receptor antagonist, IC50 = 2.49 nM. DT-9081 hydrochloride blocks PGE2/EP4R-mediated cAMP signaling, counteracts EP4R-driven immunosuppression, and restores antitumor immunity. DT-9081 hydrochloride combined with anti-PD-1 antibody significantly improves tumor growth inhibition and animal survival in mouse tumor models. DT-9081 hydrochloride can be used in cancer-related research.
For research use only. We do not sell to patients.
- Formula: C25H30ClF3N2O4
- Molecular Weight:514.96
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
EP4 2.49 nM (IC50) |
CYP2C8 11.7 μM (IC50) |
CYP2C19 3.17 μM (IC50) |
In Vitro
DT-9081 hydrochloride binds EP4R with an inhibition rate of 100.1% and is highly selective for other prostanoid receptors[1].
DT-9081 (10 μM) hydrochloride 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 hydrochloride 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) hydrochloride 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.
In Vivo
DT-9081 (30 mg/kg; p.o.; twice daily; day 8 to day 28) hydrochloride 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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Molecular Weight 514.96
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Formula C25H30ClF3N2O4
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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.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DT-9081 hydrochloride Related Classifications
HY-189816A Related Classifications
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