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YHO-13351 free base

Names

[ CAS No. ]:
912288-64-3

[ Name ]:
YHO-13351 free base

[Synonym ]:
1-{5-[(Z)-2-Cyano-2-(3,4-dimethoxyphenyl)vinyl]-2-thienyl}-4-piperidinyl N,N-diethylglycinate
Glycine, N,N-diethyl-, 1-[5-[(Z)-2-cyano-2-(3,4-dimethoxyphenyl)ethenyl]-2-thienyl]-4-piperidinyl ester
YHO-13351 (free base)

Biological Activity

[Description]:

YHO-13351 (free base) is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.IC50 value:Target: BCRP inhibitorin vitro: YHO-13177 potentiates the cytotoxicity of SN-38, mitoxantrone, and topotecan in both BCRP-transduced human colon cancer HCT116 (HCT116/BCRP) cells and SN-38-resistant human lung cancer A549 (A549/SN4) cells that express BCRP, but had little effect in the parental cells. In addition, YHO-13177 potentiates the cytotoxicity of SN-38 in human lung cancer NCI-H460 and NCI-H23, myeloma RPMI-8226, and pancreatic cancer AsPC-1 cells that intrinsically expressed BCRP. YHO-13177 increases the intracellular accumulation of Hoechst 33342, a substrate of BCRP, at 30 minutes and partially suppresses the expression of BCRP protein at more than 24 hours after its treatment in both HCT116/BCRP and A549/SN4 cells [1].in vivo: In mice, YHO-13351 is rapidly converted into YHO-13177 after its oral or intravenous administration. Coadministration of irinotecan with YHO-13351 significantly increases the survival time of mice inoculated with BCRP-transduced murine leukemia P388 cells and suppressed the tumor growth in an HCT116/BCRP xenograft model, whereas irinotecan alone has little effect in these tumor models [1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> BCRP
Research Areas >> Cancer

[References]

[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.


[Related Small Molecules]

Ko 143 | elacridar | Fumitremorgin C | KS 176 | YHO-13177 | YHO-13351 | (S)-ML753286 | Zamicastat

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
627.1±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C26H33N3O4S

[ Molecular Weight ]:
483.623

[ Flash Point ]:
333.1±31.5 °C

[ Exact Mass ]:
483.219177

[ LogP ]:
5.17

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.594

[ Storage condition ]:
2-8℃


Related Compounds