YHO-13351 (free base)

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 10mM*1mL (in DMSO)
ArtNr HY-12758A-10mM
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
YHO13351 free base, YHO 13351 free base
CAS No.
912288-64-3
Purity
>98%
MW
4836229
Formula
C26H33N3O4S
Solubility
DMSO: >= 30 mg/mL
Biological 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 inhibitor
in 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].
Free  Sample
Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 10mM*1mL (in DMSO)
Lieferbar: In stock
Listenpreis: 204,29 €
Preis: 204,29 €
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