A modulator of P-gp (Ki = 59 nM); restores the sensitivity of P-gp-expressing cancer cells to vinblastine

Zosuquidar (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
167465-36-3
Storage:
-20
UN-No:
Non-Hazardous - /

Zosuquidar is a modulator of P-glycoprotein (P-gp; Ki = 59 nM).{33874} It restores the sensitivity of P-gp-expressing cancer cells to vinblastine (Item No. 11762), doxorubicin (Item No. 15007), etoposide (Item No. 12092), and paclitaxel (Item No. 10461) when used at 0.1 µM.{33874} It less potently inhibits cytochrome P450 (CYP) isoforms CYP3A, CYP2D6, and CYP2C9 (Kis = 3.8, 25, and 12 µM, respectively).{33875} Zosuquidar does not modulate multidrug resistance-associated protein 1 (MRP-1). Zosuquidar significantly enhances the efficacy of chemotherapeutics in mice implanted with P-gp-expressing tumors.{33874} Through its effects on P-gp, zosuquidar enhances the distribution of P-gp substrates through the blood-brain barrier into the brain.{33873,33876}  

 

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Description

A modulator of P-gp (Ki = 59 nM); restores the sensitivity of P-gp-expressing cancer cells to vinblastine, doxorubicin, etoposide, and paclitaxel; enhances the distribution of P-gp substrates through the BBB into the brain

Formal name: (αR)-4-[(1aα,6α,10bα)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-α-[(5-quinolinyloxy)methyl]-1-piperazineethanol, trihydrochloride

Synonyms:  LY335979|RS 33295-198

Molecular weight: 637

CAS: 167465-36-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Cytochrome P450||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cancer|Multidrug Resistance

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