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Cat. No. Name Size Price Add Cart
KI1424LY335979 3HCl10 mg$148.5
LY335979 3HCl10 mg$220
LY335979 3HCl50 mg$1188
LY335979 3HCl100 mg$2079

Chemical Characteristic

Product NameLY335979 3HCl
SynonymsRS-33295-198, zosuquidar trihydrochloride
CAS No.167465-36-3
Molecular Weight 636.99
FormulaC32H31F2N3O2.3HCl
Chemical Name(R)-1-(4-((1aR,6s,10bS)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c][7]annulen-6-yl)piperazin-1-yl)-3-(quinolin-5-yloxy)propan-2-ol trihydrochloride
SmilesC([C@H](COc1c2cccnc2ccc1)O)N1CCN(CC1)C1c2c([C@H]3[C@@H](c4c1cccc4)C3(F)F)cccc2 Cl Cl Cl
Chemical Structure

Biological activities

LY335979 is a novel potent modulator of P-glycoprotein (Pgp). LY335979 inhibits Pgp with an IC50 of 4 nM.[1] LY335979 has a very high affinity for Pgp, with a Kd of 73 nM. LY335979 noncompetitively inhibits CYP2D6 with a Ki of 25.3 µM. LY335979 is a competitive inhibitor of CYP3A with a Ki of 3.8 µM. [2] LY335979 can effectively block Pgp function on isolated CD56+ lymphocytes and CD56+ lymphocytes in whole blood with IC50 of 1.2 and 174 nM, respectively. [3] The cytotoxic IC50 of LY335979 against CCRF-CEM, CEM/VLB100, P388, P388/ADR, MCF-7, MCF-7/ADR, 2780 and 2780 AD cell lines is 6, 7, 15, 8, 7, 15, 11 and 16 µM, respectively. LY335979 modulates Dox cytotoxicity even when LY335979 (0.5 µM) is removed 24 hours prior to the cytotoxicity assay. LY335979 blocks [3H]azidopine photoaffinity labeling of the Mr 170,000 Pgp in CEM/VLB100 plasma membranes. LY335979 competitively inhibits equilibrium binding of [3H]vinblastine to Pgp with a Ki of 0.06 µM. LY335979 enhances the survival time of mice inoculated with P388/ADR cells by 120-140%. In vivo, LY335979 reverses Pgp-mediated drug resistance in mice bearing drug-resistant variants of a murine leukemia and a human non-small cell lung carcinoma. [4]

Protocols

LY335979 is dissolved in 5% mannitol. [4]

References

[1] Harmsen S, et al. PXR-mediated induction of P-glycoprotein by anticancer drugs in a human colon adenocarcinoma-derived cell line. Cancer Chemother Pharmacol. 2010, 66(4): 765-771.
[2] Dantzig AH, et al. Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities. J Pharmacol Exp Ther. 1999, 290(2): 854-862.
[3] Green LJ, et al. Modulation by LY335979 of P-glycoprotein function in multidrug-resistant cell lines and human natural killer cells. Biochem Pharmacol. 2001, 61(11): 1393-1399.
[4] Dantzig AH, et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 1996, 56(18): 4171-4179.

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