An inhibitor of P-gp; selectively reverses multidrug resistance mediated by P-gp over MRP1- and BCRP-mediated multidrug resistance; resensitizes SKOV3TR and OVCAR-8TR cells to paclitaxel; reverses P-gp efflux

NSC 23925 – 25 mg

Brand:
Cayman
CAS:
858474-14-3
Storage:
-20
UN-No:
Non-Hazardous - /

NSC 23925 is a non-substrate inhibitor of P-glycoprotein (P-gp).{49228} It selectively reverses multidrug resistance mediated by P-gp over resistance mediated by multidrug resistance-associated protein 1 (MRP1/ABCC1) or breast cancer resistance protein (BCRP/ABCG2). It resensitizes paclitaxel-resistant SKOV3TR and OVCAR-8TR cells to paclitaxel (Item No. 10461). NSC 23925 reverses P-gp efflux, increasing the intracellular accumulation of P-gp substrates, including calcein AM (Item No. 14948) in multidrug-resistant SKOV3TR and OVCAR-8TR cells. It prevents paclitaxel-induced overexpression of the P-gp gene MDR1 and P-gp protein level increases in OVCAR-8 cells.{49229} It also prevents the development of paclitaxel-induced multidrug resistance in a SKOV3 mouse xenograft model when administered at a dose of 50 mg/kg per day in combination with paclitaxel.  

 

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Description

An inhibitor of P-gp; selectively reverses multidrug resistance mediated by P-gp over MRP1- and BCRP-mediated multidrug resistance; resensitizes SKOV3TR and OVCAR-8TR cells to paclitaxel; reverses P-gp efflux, increasing the intracellular accumulation of P-gp substrates in multidrug resistant SKOV3TR and OVCAR-8TR cells; prevents paclitaxel-induced overexpression of MDR1 and P-gp protein level increases in OVCAR-8 cells; prevents the development of paclitaxel-induced multidrug resistance in a SKOV3 mouse xenograft model at 50 mg/kg per day in combination with paclitaxel

Formal name: 2-(4-methoxyphenyl)-α-2-piperidinyl-4-quinolinemethanol, dihydrochloride

Synonyms: 

Molecular weight: 421.4

CAS: 858474-14-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cancer|Multidrug Resistance

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