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Zosuquidar (LY335979) 3HCl 167465-36-3

Product Description

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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)


Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

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
rat Km(6)







Chemical Information




Molecular Weight (MW) 636.99
Formula

C32H31F2N3O2.3HCl

CAS No. 167465-36-3

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms



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







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Product Categories : Neuronal Signaling > P-gp Inhibitor

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