MF-766 - Moligand™,10mM in DMSO , CAS No.1050656-06-8

CAS: 1050656-06-8 Cat. No.: M655089 Peso molecular: 478.46 PubChem CID: 25003075

GRADE & PURITY Moligand™, 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

MF-766 is a highly potent, selective and orally active EP4 antagonist with a K i of 0.23 nM. MF-766 behaves as a full antagonist with an IC 50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay. MF-766 can be used for cancer and inflammation diseases research

In Vitro

MF-766 (0.01-10 μM; pretreatment for 1 h and then stimulated with 50 ng/mL IL-2; with and without 0.33 μM PGE2; 18 hours) reverses PGE2-suppressed IFN-γ secretion in human NK cells. Additionally, NK cell viability is not affected by MF-766. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

MF-766 (oral gavage; 30 mg/kg; once daily; 21 days) exhibits TGI% of 49% in CT26 tumor model. But it does not exhibits significant difference in EMT6 and 4T1 tumor model. MF-766 (oral gavage; 30 mg/kg combination with anti-PD-1 mDX400; once daily; 21 days; q4dx8) shows potent anti-tumor activities in different preclinical models. The % of TGI are 89%, 66% and 40%, respectively in CT26 tumor, EMT6 and 4T1 tumor model. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female C57BL/6 J strain mice injected subcutaneously with CT26, EMT6, or 4T1 cellsDosage: 30 mg/kg combination with anti-PD-1 mDX400 Administration: Oral gavage; 10 mg/kg or 30 mg/kg combination with anti-PD-1 mDX400; once daily; 21 days; q4dx8 Result: Improved anti-tumor activity in the setting of PD-1 blockade in multiple syngeneic models.

IC50& Target:EP4 0.23 nM (Ki)

Specifications

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

MF-766 is a highly potent, selective and orally active EP4 antagonist with a K i of 0.23 nM. MF-766 behaves as a full antagonist with an IC 50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay. MF-766 can be used for cancer a

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Grado

Moligand™

Tipo de acción

ANTAGONIST

Nombres e identificadores

• Isómeros SMILES: C1CC1(C2=CC=C(C=C2)C(=O)O)NC(=O)C3=CC=CC4=C3N(C=C4)CC5=CC=C(C=C5)C(F)(F)F
• CAS alternativo: 1050656-06-8
• PubChem CID: 25003075
• Peso molecular: 478.46

Objetivos asociados (humanos)

PTGER4 Tclin Prostaglandin E2 receptor EP4 subtype (5 Activities)

Discover Target: PTGER4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)