MF-766

小分子

EX-A5897 | BDBM50319837 | AKOS040759910 | 4-[1-[[1-[[4-(trifluoromethyl)phenyl]methyl]indole-7-carbonyl]amino]cyclopropyl]benzoic acid | MF766 | MF-766 | 86KF5VSV88 | 4-{1-[({1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl}carbonyl)amino]cyclopropyl}benzoic A

MF-766

M647575-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

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. Form:Solid IC50& Target:EP4 0.23 nM (Ki)

MF-766 是一种强效、选择性和口服活性 EP4 拮抗剂，其 K i 为 0.23 nM。在功能测试中，MF-766 表现为完全拮抗剂，IC 50 为 1.4 nM（在存在 10% HS 的情况下升至 1.8 nM）。MF-766可用于癌症的拮抗剂研究。

1050656-06-8

C27H21F3N2O3

478.46 g/mol

25003075

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

4-[1-[[1-[[4-(trifluoromethyl)phenyl]methyl]indole-7-carbonyl]amino]cyclopropyl]benzoic acid

1S/C27H21F3N2O3/c28-27(29,30)21-8-4-17(5-9-21)16-32-15-12-18-2-1-3-22(23(18)32)24(33)31-26(13-14-26)20-10-6-19(7-11-20)25(34)35/h1-12,15H,13-14,16H2,(H,31,33)(H,34,35)

BWXAZFCPGFKANL-UHFFFAOYSA-N

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

25003075

1050656-06-8

DMSO : 50 mg/mL (104.50 mM; Need ultrasonic)

2

6

6

478.15 Da

478.15 Da

71.300 Ų

35

0

783.000

0

1

5.100