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首页-小分子抑制剂&激动剂-GPCR-Prostaglandin Receptor-KF-0210
KF-0210

Chemical Structure : KF-0210

CAS No.: 2455480-28-9

KF-0210 (KF0210)

货号: PC-28214Not For Human Use, Lab Use Only.

KF-0210 is a potent, selective and oral EP4 receptor antagonist with binding IC50 of 18.6 nM, shows >500-fold selectivity over other prostaglandin receptors, including EP1, EP2, EP3, IP, DP1, and FP.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

KF-0210 is a potent, selective and oral EP4 receptor antagonist with binding IC50 of 18.6 nM, shows >500-fold selectivity over other prostaglandin receptors, including EP1, EP2, EP3, IP, DP1, and FP.
KF-0210 increases LPS-induced TNFα release (IC50=4.5 nM) in the presence of PGE2 in human PBMCs.
KF-0210 inhibits PGE2-induced cAMP production with IC50 of 1.06 nM in MCF-7 cells and 0.915 nM in Flpin-293-mEP4 cells.
KF-0210 increases the tumor-killing immune cells in the tumor in CT26 mouse model of colorectal cancer.
Combination treatment of KF-0210 and PD-1/PD-L1 antibodies shows a superior therapeutic effect compared to the monotherapy of each treatment.

物理化学性质&存储条件

分子量 440.50
分子式 C27H24N2O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Bicyclo[1.1.1]pentane-1-carboxylic acid, 3-[1-[[[1-(2-benzofuranylmethyl)-1H-indol-7-yl]carbonyl]amino]cyclopropyl]-

参考文献

1. Yongqi Deng, et al. Cancer Res (2023) 83 (7_Supplement): 2330.

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