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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Aryl hydrocarbon Receptor (AhR)-IK-175
IK-175

Chemical Structure : IK-175

CAS No.: 2247950-42-9

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IK-175 (IK175)

货号: PC-38860Not For Human Use, Lab Use Only.

IK-175 is a potent, selective and orally active aryl hydrocarbon receptor (AHR) antagonist with IC50 of 91 nM in human HepG2 cells expressing an AHR-dependent DRE-luciferase reporter and stimulated with 80 nM of the AHR agonist VAF347.

规格 价格 库存 数量
2 mg ￥1980 In stock
5 mg ￥2980 In stock
10 mg ￥4580 In stock
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纯度 & COA & 质检文件 纯度: 99.30% (HPLC) Select Batch:

生物&药学活性

IK-175 is a potent, selective and orally active aryl hydrocarbon receptor (AHR) antagonist with IC50 of 91 nM in human HepG2 cells expressing an AHR-dependent DRE-luciferase reporter and stimulated with 80 nM of the AHR agonist VAF347.
IK-175 inhibits AHR activity in experimental systems derived from multiple species including mouse, rat, monkey, and humans.
IK-175 inhibits AHR activity in rodent and human cancer cell lines as well as human and nonhuman primate primary immune cells, with concentration dependent effects on AHR target gene expression and cytokine release.
Orally administered IK-175 dose-dependently blocks ligand stimulated-AHR activation of Cyp1a1 transcription in liver and spleen, demonstrating on-target in vivo activity in mice.
IK-175 alone and in combination with an anti-PD-1 antibody demonstrates significant antitumor activity in syngeneic mouse models of colorectal cancer (CT26.WT) and melanoma (B16-IDO1).

物理化学性质&存储条件

分子量 441.514
分子式 C25H24FN7
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

(R)-N-(2-(5-fluoropyridin-3-yl)-8-isopropylpyrazolo[1,5-a][1,3,5]triazin-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-amine

参考文献

1. Karen McGovern, et al. Mol Cancer Ther. 2022 Jun 6;molcanther.0984.2021-12-8 12:58:05.173.

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