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)
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.
Chemical Information
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Contact us if you need more details on 167465-36-3 Zosuquidar 3HCl 167465-36-3. We are ready to answer your questions on packaging, logistics, certification or any other aspects about LY335979 3HCl 167465-36-3、167465-36-3. If these products fail to match your need, please contact us and we would like to provide relevant information.
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 |
---|
Molarity Calculator
Dilution Calculator
Molecular Weight Calculator
Contact us if you need more details on 167465-36-3 Zosuquidar 3HCl 167465-36-3. We are ready to answer your questions on packaging, logistics, certification or any other aspects about LY335979 3HCl 167465-36-3、167465-36-3. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : Neuronal Signaling > P-gp Inhibitor
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