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Purity: ≥98%
Zosuquidar 3HCl (formerly D-06387; D06387; RS33295198; LY335979; LY-335979; RS-33295198), the trihydrochloride salt of zosuquidar, is a novel and potent inhibitor P-glycoprotein (P-gp) and modulator of P-gp-mediated multi-drug resistance with potential antitumor activity. It inhibits P-gp with a Ki of 60 nM in a cell-free assay.
| ln Vitro |
In P-glycoprotein-active cell lines, zosuquidar (0.3 μM; 48 h) increases the cytotoxicity of DNR (substrates for P-glycoproteins)[2]. Drug-sensitive and multidrug-resistant cell lines exhibit high cytotoxic concentrations when treated with zosuquidar (5–16 μM) for 72 hours[1].
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| ln Vivo |
Treatment with zosuquidar (intraperitoneal injection; 30, 10, 3, or 1 mg/kg; once daily; 5 d) significantly lengthens life[1]. ?Doxorubicin combined with Zosuquidar (intraperitoneal injection; 30 mg/kg; once daily; 5 d) treatment demonstrates potentiation[1].
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| Cell Assay |
Cell Cytotoxicity Assay[2]
Cell Types: K562 and HL60 cells Tested Concentrations: 0.3 μM Incubation Duration: 48 hrs (hours) Experimental Results: Enhanced the cytotoxicity of DNR (substrates for P-glycoproteins) in K562/DOX cells more than 45.5-fold. Cell Cytotoxicity Assay[1] Cell Types: CCRF-CEM, CEM/VLB100, P388, P388/ADR, MCF7, MCF7/ADR, 2780, 2780AD, UCLA-P3, UCLA-P3.003VLB cells Tested Concentrations: 5-16 μM Incubation Duration: 72 hrs (hours) Experimental Results: demonstrated IC50s of 6, 7, 15, 8, 7, 15, 11, 16, >5, >5 μM for CCRF-CEM, CEM/VLB100, P388, P388 /ADR, MCF7, MCF7/ADR, 2780, 2780AD, UCLA-P3, UCLA-P3.003VLB cells, respectively. |
| Animal Protocol |
Animal/Disease Models: Mice implanted with P388/ADR tumors[1]
Doses: 30, 10, 3, or 1 mg/kg Route of Administration: intraperitoneal (ip)injection; 30, 10, 3, or 1 mg/kg; one time/day; 5 days Experimental Results: Exihibited a Dramatically increased survival compared to the group treated with Doxorubicin alone (P<0.001). Animal/Disease Models: Mice implanted with P388 or P388/ADR murine leukemia cells[1] Doses: 30 mg/kg Route of Administration: intraperitoneal (ip)injection; 30 mg/kg; one time/day; 5 days Experimental Results: Observed significant antitumor activity against the MDR P388/ADR cell lines when mice were treated with a combined dose of 30 mg/kg LY335979 and 1 mg/kg Doxorubicin (P=0.1). |
| References |
[1]. A H Dantzig, et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 1996 Sep 15;56(18):4171-9.
[2]. Ruoping Tang, et al. Zosuquidar restores drug sensitivity in P-glycoprotein expressing acute myeloid leukemia (AML). BMC Cancer. 2008 Feb 13;8:51. [3]. Larry D Cripe, et al. Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999. Blood. 2010 Nov 18;116(20):4077-85. |
| Molecular Formula |
C32H31F2N3O2.3HCL
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| Molecular Weight |
636.99
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| CAS # |
167465-36-3
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| Related CAS # |
167354-41-8
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| SMILES |
Cl[H].Cl[H].Cl[H].FC1([C@@]2([H])C3=C([H])C([H])=C([H])C([H])=C3C([H])(C3=C([H])C([H])=C([H])C([H])=C3[C@]21[H])N1C([H])([H])C([H])([H])N(C([H])([H])[C@]([H])(C([H])([H])OC2=C([H])C([H])=C([H])C3=C2C([H])=C([H])C([H])=N3)O[H])C([H])([H])C1([H])[H])F
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5699 mL | 7.8494 mL | 15.6988 mL | |
| 5 mM | 0.3140 mL | 1.5699 mL | 3.1398 mL | |
| 10 mM | 0.1570 mL | 0.7849 mL | 1.5699 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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