ZOSUQUIDAR TRIHYSROCHLORIDE Property

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

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H226Flammable liquid and vapour

H314Causes severe skin burns and eye damage

Precautionary statements

P210Keep away from heat/sparks/open flames/hot surfaces. — No smoking.

P233Keep container tightly closed.

P240Ground/bond container and receiving equipment.

P241Use explosion-proof electrical/ventilating/lighting/…/equipment.

P242Use only non-sparking tools.

P243Take precautionary measures against static discharge.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P330+P331IF SWALLOWED: Rinse mouth. Do NOT induce vomiting.

P303+P361+P353IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.

P370+P378In case of fire: Use … for extinction.

P403+P235Store in a well-ventilated place. Keep cool.

P405Store locked up.

ZOSUQUIDAR TRIHYSROCHLORIDE Chemical Properties,Usage,Production

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].

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.