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Chemical Structure| 167465-36-3 Chemical Structure| 167465-36-3

Structure of Zosuquidar 3HCl
CAS No.: 167465-36-3

Chemical Structure| 167465-36-3

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Zosuquidar (LY335979) trihydrochloride is a P-glycoprotein (P-gp) inhibitor with a Ki of 59 nM. It shows anti-tumor activities and can be used in acute myelogenous leukemia (AML) research.

Synonyms: LY-335979 trihydrochloride; RS 33295-198 trihydrochloride; RS 33295-198

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Product Details of Zosuquidar 3HCl

CAS No. :167465-36-3
Formula : C32H34Cl3F2N3O2
M.W : 636.99
SMILES Code : FC1([C@H]2[C@@H]1C3=C([C@@H](C4=CC=CC=C42)N5CCN(CC5)C[C@H](COC6=C7C=CC=NC7=CC=C6)O)C=CC=C3)F.Cl.Cl.Cl
Synonyms :
LY-335979 trihydrochloride; RS 33295-198 trihydrochloride; RS 33295-198
MDL No. :MFCD00942300
InChI Key :ZPFVQKPWGDRLHL-ZLYBXYBFSA-N
Pubchem ID :153997

Safety of Zosuquidar 3HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • P-gp

    P-gp, Ki:60 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
NCI-H1299 10 ×10−6m 24 hours Zosuquidar significantly suppresses PD-L1 expression PMC11538701
NCI-H460 2.5 ×10−6m, 5 ×10−6m, 10 ×10−6m 24 hours Zosuquidar down-regulates PD-L1 expression in a dose-dependent manner PMC11538701
NCI-H1975, SKOV3, 786-O, MIA PaCa-2 10 ×10−6m 24 hours Zosuquidar reduces PD-L1 expression in multiple cancer cell lines PMC11538701
22Rv1 AUR-3 cells 1 µM 4 hours Restored AU-15330 degradation efficacy in 22Rv1 AUR-3 cells PMC11009648
22Rv1 AUR-3 cells 1 µM Restored sensitivity of 22Rv1 AUR-3 cells to other PROTAC degraders PMC11009648
MDCK-MDR1 cells 1 μM 60 minutes restored pazopanib cellular accumulation and abolished the directionality of pazopanib flux PMC3573846

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice C57Bl6 mice Oral 24 days To study the impact of gut microbiota on TAC pharmacokinetics by inhibiting ABCB1A functionality, results showed that ZSQ supplementation significantly increased TAC whole blood exposure PMC10324113
Mouse CT26 mouse model Oral 60 mg/kg Once daily for 2-6 weeks Zosuquidar significantly suppresses tumor growth and increases infiltration of cytotoxic T cells PMC11538701
mice 22Rv1 AUR-3 CDX model intraperitoneal injection 30 mg/kg Single dose Restored AU-15330 degradation efficacy in 22Rv1 AUR-3 tumors PMC11009648
FVB wild type mice FVB wild type mice intravenously 10 mg/kg, 20 mg/kg, 40 mg/kg daily 5 d per week for 5 d to investigate the effect of P-gp inhibition on pazopanib brain accumulation, results showed that zosuquidar alone did not significantly alter pazopanib brain accumulation PMC3573846

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00046930 Leukemia Myel... More >>odysplastic Syndromes Less << Phase 3 Completed - -
NCT00046930 - Completed - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.57mL

0.31mL

0.16mL

7.85mL

1.57mL

0.78mL

15.70mL

3.14mL

1.57mL

References

 

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