| Identification | Back Directory | [Name]
ZOSUQUIDAR TRIHYSROCHLORIDE | [CAS]
167465-36-3 | [Synonyms]
CS-58
D06387
LY335979
RS 33295-198
Zosuquidar 3HCl
Trihydrochloride
Zosuquidar TriHCl
Zosuquidar (LY335979
LY335979, RS 33295-198
RS-33295-198, ZOSUQUIDAR
Zosuquidr.3HCl(LY335979)
Zosuquidar (LY335979) 3HCl
LY-335979 trihydrochloride
RS 33295-198 (D06387) 3HCl
LY335979 (Zosuquidar 3HCl)
ZOSUQUIDAR TRIHYSROCHLORIDE
Zosuquidar Trihydrochloride
RS 33295-198 trihydrochloride
Zosuquidar trihydrochloride, >=98%
RS-33295-198; ZOSUQUIDAR; LY-335979
ZOSUQUIDAR TRIHYSROCHLORIDE USP/EP/BP
Zosuquidar (LY335979) triHydrochloride
LY335979 (Zosuquidar trihydrochloride)
Zosuquidar trihydrochloride
LY335979
LY 335979; LY-335979; LY335979; D06387; RS33295198;
(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 Hydrochloride
1-Piperazineethanol, 4-[(1aα,6α,10bα)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-α-[(5-quinolinyloxy)methyl]-,trihydrochloride
(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
(2R)-1-{4-[(1aR,6r,10bS)-1,1-Difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]piperazin-1-yl}-3-(quinolin-5-yloxy)propan-2-ol trihydrochloride
1-Piperazineethanol,4-[(1aa,6a,10ba)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-a-[(5-quinolinyloxy)methyl]-,hydrochloride (1:3), (aR)-
(2R)-1-{4-[(1aR,6r,10bS)-1,1-Difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]piperazin-1-yl}-3-(quinolin-5-yloxy)propan-2-ol trihydrochloride Zosuquidar trihydrochloride LY335979
[6(R)-(1aα,6α,10bα)]-4-(1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl)-α-[(5-quinolinyloxy)Methyl]-piperazineethanol trihydrochloride, (2R)-anti-5-{3-[4-(10,11-difluoroMethanodibenzosuber-5-yl)piperazin-1-yl]-2-hydroxypropoxy | [Molecular Formula]
C32H31F2N3O2.3ClH | [MDL Number]
MFCD24369599 | [MOL File]
167465-36-3.mol | [Molecular Weight]
636.995 |
| Chemical Properties | Back Directory | [Melting point ]
172-176°C | [storage temp. ]
Inert atmosphere,Room Temperature | [solubility ]
Methanol (Slightly), Water (Slightly, Sonicated) | [form ]
Solid | [color ]
Pale Yellow to Light Yellow |
| Hazard Information | Back Directory | [Chemical Properties]
Pale Yellow Solid | [Uses]
Multi-drug resistance (MDR) modulator; selective inhibitor of P-glycoprotein (P-gp). Antineoplastic adjunct (chemosensitizer). | [Biological Activity]
ly335979 is a selective inhibitor of p-gp with ic50 value of 1.2 nm [1, 2].p-gp (p-glycoprotein) is a member of atp-binding cassette (abc) transporters and plays a pivotal role in pumping many foreign substances out of cells. it has been reported that abnormal expression of p-gp is correlated with the multidrug resistance of tumor cells [3].ly335979 is a potent p-gp inhibitor and has a different selectivity with the reported p-gp inhibitor cyclosporin a or verapamil. in drug-resistant cell line hl60/vcr with highly expression of p-gp, ly335979 exhibited highly restore ability of p-gp than cyclosporin a or verapamil and the ic 50 value of 1.2 nm [1]. when tested with a panel of cell lines over-expressed p-gp (cem/vlb100, mcf-7/adr, 2780ad, p388/adr, and ucla-p3.003vlb), administration of ly335979 reversed the cells resistance to vinblastine, doxorubicin, btoposide and taxol by inhibiting p-gp activity [2].in female nude mice model with ucla-p3.003vlb mdr tumor cells subcutaneous xenograft, pre-treated with ly335979 (30mg/kg) restored tumor cells sensitivity to taxol (20 mg/kg) which combination markedly suppressed solid tumor growth compared with control group [2]. | [storage]
Store at -20°C | [References]
1. green, l.j., p. marder, and c.a. slapak, modulation by ly335979 of p-glycoprotein function in multidrug-resistant cell lines and human natural killer cells. biochem pharmacol, 2001. 61(11): p. 1393-9.2. dantzig, a.h., et al., reversal of p-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, ly335979. cancer res, 1996. 56(18): p. 4171-9.3. hu, t., et al., reversal of p-glycoprotein (p-gp) mediated multidrug resistance in colon cancer cells by cryptotanshinone and dihydrotanshinone of salvia miltiorrhiza. phytomedicine, 2014. 21(11): p. 1264-72. |
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