VER-50589

Bezeichnung:VER-50589

CAS-Nr747413-08-7

Englisch Name:VER-50589

CBNumberCB32592830

SummenformelC19H17ClN2O5

Molgewicht388.8

MOL-Datei747413-08-7.mol

VER-50589 physikalisch-chemischer Eigenschaften

Siedepunkt	583.0±50.0 °C(Predicted)
Dichte	1.360±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	≥38.9 mg/mL in DMSO; insoluble in H2O; ≥57.2 mg/mL in EtOH
pka	7.12±0.25(Predicted)
Aggregatzustand	solid
Farbe	White to off-white

VER-50589 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
VER-50589 inhibits the intrinsic ATPase activity of recombinant yeast Hsp90. It produces antiproliferative activity in a panel of human cancer cell lines and nontumorigenic cells in vitro.
Biologische Aktivität
ver-50589 is a potent inhibitor of hsp90 with ic50 value of 21 nm for hsp90β [1].heat shock protein 90 (hsp90) is a chaperone protein that stabilizes proteins against heat stress, assists proteins to fold properly and aids in protein degradation. also, hsp90 stabilizes proteins required for tumor growth.ver-50589 is a potent hsp90 inhibitor. ver-50589 inhibited recombinant yeast hsp90 atpase activity with ic50 value of 143 nm at 400 μm atp and inhibited recombinant human hsp90β with ic50 value of 821 nm in the presence of the activator aha1. also, ver-50589 bound to recombinant human hsp90β with kd value of 4.5 nm. in human cancer cells, ver-50589 exhibited antiproliferative activity with mean gi50 value of 78 nm. in ch1 human ovarian cells, ver-50589 inhibited cell growth with gi50 value of 32.7 nm. in ht29 cells, ver-50589 exhibited extensive glucuronidation and increased glucuronide levels by 50-fold, which were responsible for the resistance. in ch1doxr cells that were resistant to doxorubicin, ver-50589 exhibited similar cellular gi50 value compared with ch1 cells. in hct116 colon cancer cells, ver-50589 caused g1 and g2-m block. also, ver-50589 induced cytostasis and apoptosis [1].in athymic mice bearing ovcar3 human ovarian ascites tumors, ver-50589 completely inhibited hsp90. in mice bearing hct116 colon carcinoma xenografts, ver-50589 (100 mg/kg) reduced tumor volume by 30% and tumor weight by 26%. also, ver-50589 reduced expression of erbb2 and c-raf [1].
target
HSP90β
Einzelnachweise
[1]. sharp sy, prodromou c, boxall k, et al. inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues. mol cancer ther, 2007, 6(4): 1198-1211.

VER-50589 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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