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| | ZOSUQUIDAR TRIHYSROCHLORIDE Basic information |
| | 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. |
| | ZOSUQUIDAR TRIHYSROCHLORIDE Preparation Products And Raw materials |
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