IK-175 is an oral, selective, small molecule Aryl Hydrocarbon Receptor (AHR) inhibitor. 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. IK-175 is inactive in a broad panel of kinases, receptors, and transporters. 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). In addition, IK-175 in combination with liposomal doxorubicin demonstrates antitumor activity in syngeneic mouse models of colorectal cancer
MedKoo Cat#: 207221
Name: IK-175
CAS#: 2247950-42-9
Chemical Formula: C25H24FN7
Exact Mass: 441.2077
Molecular Weight: 441.51
Elemental Analysis: C, 68.01; H, 5.48; F, 4.30; N, 22.21
The following data is based on the product molecular weight 441.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
