ZOSUQUIDAR TRIHYSROCHLORIDE
ZOSUQUIDAR TRIHYSROCHLORIDE Basic information
- Product Name:
- ZOSUQUIDAR TRIHYSROCHLORIDE
- Synonyms:
-
- Zosuquidar 3HCl
- Zosuquidar trihydrochloride, >=98%
- Trihydrochloride
- Zosuquidar (LY335979) triHydrochloride
- D06387
- LY 335979; LY-335979; LY335979; D06387; RS33295198;
- (αR)-4-[(1aα,6α,10bα)-1,1-Difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-α-[(5-quinolinyloxy)methyl]-1-piperazineethanol trihydrochloride
- RS-33295-198; ZOSUQUIDAR; LY-335979
- CAS:
- 167465-36-3
- MF:
- C32H32ClF2N3O2
- MW:
- 564.07
- Product Categories:
-
- Inhibitors
- Aromatics
- Chiral Reagents
- Heterocycles
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Mol File:
- 167465-36-3.mol
ZOSUQUIDAR TRIHYSROCHLORIDE Chemical Properties
- Melting point:
- 172-176°C
- storage temp.
- Inert atmosphere,Room Temperature
- solubility
- Methanol (Slightly), Water (Slightly, Sonicated)
- form
- Solid
- color
- Pale Yellow to Light Yellow
- InChIKey
- VQJFFWJUYDGTQZ-NMTXSAMUNA-N
- SMILES
- FC1([C@H]2C3C=CC=CC=3[C@H](N3CCN(C[C@@H](O)COC4C=CC=C5N=CC=CC=45)CC3)C3C=CC=CC=3[C@@H]12)F.Cl |&1:2,9,15,37,r|
ZOSUQUIDAR TRIHYSROCHLORIDE Usage And Synthesis
Chemical Properties
Pale Yellow Solid
Uses
Multi-drug resistance (MDR) modulator; selective inhibitor of P-glycoprotein (P-gp). Antineoplastic adjunct (chemosensitizer).
Biological Activity
ly335979 is a selective inhibitor of p-gp with ic50 value of 1.2 nm [1, 2].p-gp (p-glycoprotein) is a member of atp-binding cassette (abc) transporters and plays a pivotal role in pumping many foreign substances out of cells. it has been reported that abnormal expression of p-gp is correlated with the multidrug resistance of tumor cells [3].ly335979 is a potent p-gp inhibitor and has a different selectivity with the reported p-gp inhibitor cyclosporin a or verapamil. in drug-resistant cell line hl60/vcr with highly expression of p-gp, ly335979 exhibited highly restore ability of p-gp than cyclosporin a or verapamil and the ic 50 value of 1.2 nm [1]. when tested with a panel of cell lines over-expressed p-gp (cem/vlb100, mcf-7/adr, 2780ad, p388/adr, and ucla-p3.003vlb), administration of ly335979 reversed the cells resistance to vinblastine, doxorubicin, btoposide and taxol by inhibiting p-gp activity [2].in female nude mice model with ucla-p3.003vlb mdr tumor cells subcutaneous xenograft, pre-treated with ly335979 (30mg/kg) restored tumor cells sensitivity to taxol (20 mg/kg) which combination markedly suppressed solid tumor growth compared with control group [2].
in vivo
Zosuquidar (intraperitoneal injection; 30, 10, 3, or 1 mg/kg; once daily; 5 d) treatment shows a significant increase in life span[1].
?
Zosuquidar (intraperitoneal injection; 30 mg/kg; once daily; 5 d) treatment shows the potentiation with a combined of Doxorubicin[1].
| Animal Model: | Mice implanted with P388/ADR tumors[1] |
| Dosage: | 30, 10, 3, or 1 mg/kg |
| Administration: | Intraperitoneal injection; 30, 10, 3, or 1 mg/kg; once daily; 5 days |
| Result: | Exihibited a significantly increased survival compared to the group treated with Doxorubicin alone (P<0.001). |
| Animal Model: | Mice implanted with P388 or P388/ADR murine leukemia cells[1] |
| Dosage: | 30 mg/kg |
| Administration: | Intraperitoneal injection; 30 mg/kg; once daily; 5 days |
| Result: | 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). |
storage
Store at -20°C
References
1. green, l.j., p. marder, and c.a. slapak, modulation by ly335979 of p-glycoprotein function in multidrug-resistant cell lines and human natural killer cells. biochem pharmacol, 2001. 61(11): p. 1393-9.2. dantzig, a.h., et al., reversal of p-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, ly335979. cancer res, 1996. 56(18): p. 4171-9.3. hu, t., et al., reversal of p-glycoprotein (p-gp) mediated multidrug resistance in colon cancer cells by cryptotanshinone and dihydrotanshinone of salvia miltiorrhiza. phytomedicine, 2014. 21(11): p. 1264-72.
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