In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Zosuquidar (LY335979) 3HCl is a novel and potent modulator of P-glycoprotein (P-gp) . P-gp is wildly expressed in brain, liver, small intestine and tumor cells and acts as an efflux pump responsible for multidrug resistance in tumor cells. Overexpression of Pgp in tumors results in multidrug resistance (MDR) to structurally unrelated oncolytics .
In vitro: In CEM/VLB100 cells, LY335979 treatment (0.1 μM) fully restored the sensitivity to vinblastine, doxorubicin (Dox), etoposide, and Taxol. In CEM/VLB100 plasma membranes, LY335979 blocked [3H]azidopinephotoaffinity labeling of the M(r) approximately 170,000 Pgp and competitively inhibited equilibrium binding of [3H]vinblastine to Pgp with the Ki value of approximately 0.06 μM . In all P-gp-expressing leukemia cell linesincluding K562/HHT40, K562/HHT90, K562/DOX and HL60/DNR, Zosuquidar completely or partially restored drug sensitivity. In primary AML blasts with active P-gp, Zosuquidar enhanced the cytotoxicity of anthracyclines (daunorubicin, idarubicin, mitoxantrone) and gemtuzumabozogamicin (Mylotarg).
In vivo: In mice bearing P388/ADR murine leukemia cells,treatment with LY335979 in combination with Dox or etoposide significantly increased in life span with no apparent alteration of pharmacokinetics. In a MDR human non-small cell lung carcinoma nude mouse xenograft model, LY335979 enhanced the antitumor activity of Taxol .
Clinical trials: In patients with untreated non-Hodgkin's lymphoma,a phase I/II trial was conducted to investigate the safety and tolerance of zosuquidar. In patients giving three doses of 500 mg of zosuquidar p.o. in combination with CHOX, toxicity was minimal and no enhancement of CHOP-related toxicity was observed . In patients with advanced solid tumours in Phase I study, zosuquidar(100–300 mg/m2) can inhibit vinorelbine clearance to a modest degree.
 Cripe L D, Uno H, Paietta E M, 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[J]. Blood, 2010, 116(20): 4077-4085.
 Chaudhary P M, Roninson I B. Expression and activity of P-glycoprotein, a multidrug efflux pump, in human hematopoietic stem cells[J]. Cell, 1991, 66(1): 85-94.
 Dantzig A H, Shepard R L, Cao J, et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979[J]. Cancer Research, 1996, 56(18): 4171-4179.
 Tang R, Faussat A M, Perrot J Y, et al. Zosuquidar restores drug sensitivity in P-glycoprotein expressing acute myeloid leukemia (AML)[J]. BMC cancer, 2008, 8(1): 1.
 Morschhauser F, Zinzani P L, Burgess M, et al. Phase I/II trial of a P-glycoprotein inhibitor, Zosuquidar. 3HCl trihydrochloride (LY335979), given orally in combination with the CHOP regimen in patients with non-Hodgkin's lymphoma[J]. Leukemia & lymphoma, 2007, 48(4): 708-715.
 Lê L H, Moore M J, Siu L L, et al. Phase I study of the multidrug resistance inhibitor zosuquidar administered in combination with vinorelbine in patients with advanced solid tumours[J]. Cancer chemotherapy and pharmacology, 2005, 56(2): 154-160.
|Storage||Store at -20°C|
|Solubility||Soluble in DMSO|
|Canonical SMILES||FC1([[email protected]@](C2=C([H])C([H])=C([H])C([H])=C23)([H])[[email protected]]1([H])C4=C([H])C([H])=C([H])C([H])=C4C3([H])N5C([H])([H])C([H])([H])N(C([H])([H])[[email protected]@](C([H])([H])OC6=C([H])C([H])=C([H])C7=C6C([H])=C([H])C([H])=N7)([H])O[H])C([H])([H])C5([H])[H])F|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.|
|General tips||For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.|