Molecular Weight: 636.99 Zosuquidar (LY335979) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.
LY335979 competitively inhibits equilibrium binding of [3H]vinblastine to Pgp by blocking [3H]azidopine photoaffinity labeling of the Pgp in CEM/VLB100 plasma membranes. LY335979 alone shows the cytotoxicity to drug-sensitive and MDR cell
lines with IC50 ranging from 6 μM-16 μM and produces its ability to
completely reverse the resistance of the oncolytics (vinblastine,
doxorubicin, or etoposide) to the MDR cell lines P388/ADR, MCF7/ADR,
2780AD, or UCLA-P3.003VLB at concentration of 0.1 and 0.5 μM.
LY335979 significantly restores drug sensitivity in P-gp-expressing
leukemia cell lines including K562/HHT40, K562/HHT90, K562/DOX and
HL60/DNR, and enhances the cytotoxicity of anthracyclines (daunorubicin,
idarubicin, mitoxantrone) and gemtuzumab ozogamicin (Mylotarg) in
primary AML blasts with active P-gp. A latest paper
indicates that LY335979 completely inhibits apically directed transport
of (Z)-endoxifen in the ABCB1-transduced cells.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
|Body Surface Area (m2)||0.6||0.5||0.24||0.15||0.05||0.025||0.02||0.007|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×||mouse Km(3)||= 11.2 mg/kg|
|Molecular Weight (MW)||636.99|
|Storage||3 years -20℃Powder|
|6 months-80℃in solvent (DMSO, water, etc.)|
|Solubility (25°C) *||In vitro||DMSO||100 mg/mL (156.98 mM)|
|Water||23 mg/mL (36.1 mM)|
|Ethanol||<1 mg/mL (|
|In vivo||30% PEG400/0.5% Tween80/5% propylene glycol||30 mg/mL|
|Chemical Name||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|
Molecular Weight Calculator
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