YHO-13177

YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model[1][2][3].

Product Specifications

CAS Number

[912287-56-0]

UNSPSC

12352005

Hazard Statement

H302, H312, H332

Target

BCRP

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/YHO-13177.html

Purity

99.65

Solubility

DMSO : 33.33 mg/mL (ultrasonic)

Smiles

N#C/C(C1=CC=C(OC)C(OC)=C1)=C\C2=CC=C(N3CCC(O)CC3)S2

Molecular Formula

C20H22N2O3S

Molecular Weight

370.47

Precautions

H302, H312, H332

References & Citations

[1]Yamazaki R, et al. Novel acrylonitrile derivatives, YHO-13177 and YHO-13351, reverse BCRP/ABCG2-mediated drug resistance in vitro and in vivo. Mol Cancer Ther. 2011 Jul;10 (7) :1252-63.|[2]Shishido Y, et al. ABCG2 inhibitor YHO-13351 sensitizes cancer stem/initiating-like side population cells to irinotecan. Anticancer Res. 2013 Apr;33 (4) :1379-86. |[3]Yu S, et al. The mechanisms of multidrug resistance of breast cancer and research progress on related reversal agents. Bioorg Med Chem. 2023 Nov 15;95:117486.