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129716-45-6

129716-45-6 Structure

129716-45-6 Structure
IdentificationBack Directory
[Name]

MS 073
[CAS]

129716-45-6
[Synonyms]

MS 073
CP-162398
1-Piperazineethanol, 4-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl)-α-[(5-quinolinyloxy)methyl]-
1-(Quinolin-5-yloxy)-3-[4-[(10,11-dihydro-5H-dibenzo[a,d]cyclohepten)-5-yl]piperazin-1-yl]-2-propanol
[Molecular Formula]

C31H33N3O2
[MDL Number]

MFCD00891854
[MOL File]

129716-45-6.mol
[Molecular Weight]

479.61
Hazard InformationBack Directory
[Description]

MS-073, also known as CP-162398, is a P-glycoprotein inhibitor (P-gp). MS-073 was compared with verapamil with regard to its ability to overcome MDR in vitro and in vivo. MS-073 at 0.1 microM almost completely reversed in vitro resistance to vincristine (VCR) in VCR-resistant P388 cells. MS-073 also reversed in vitro VCR, adriamycin (ADM), etoposide, and actinomycin D resistance in ADM-resistant human myelogenous leukemia K562 (K562/ADM) cells, MS-073 reverses MDR by competitively inhibiting drug binding to P-glycoprotein.
[Uses]

MS-073 (CP162398) is a P-glycoprotein (P-gp) inhibitor. MS-073 reverses multidrug resistance in drug-resistant cells by competitively inhibiting drug binding to P-glycoprotein[1][2].
[References]

[1] Sato W, et al. Circumvention of multidrug resistance by a newly synthesized quinoline derivative, MS-073[J]. Cancer research, 1991, 51(9): 2420-2424. PMID:1673087
[2] Smith B J, et al. P-glycoprotein efflux at the blood-brain barrier mediates differences in brain disposition and pharmacodynamics between two structurally related neurokinin-1 receptor antagonists[J]. Journal of Pharmacology and Experimental Therapeutics, 2001, 298(3): 1252-1259. PMID:11504828
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