|PF-04929113 (SNX-5422)Hsp90 inhibitor,potent and selective|
Sample solution is provided at 25 µL, 10mM.
Publications citing ApexBio Products
|Description||PF-04929113 is a potent and selective inhibitor of Hsp90 with IC50 value of 50 nM.|
|Cas No.||908115-27-5||SDF||Download SDF|
|Chemical Name||[4-[2-carbamoyl-5-[6,6-dimethyl-4-oxo-3-(trifluoromethyl)-5,7-dihydroindazol-1-yl]anilino]cyclohexyl] 2-aminoacetate|
|Solubility||Soluble in DMSO > 10 mM||Storage||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
PF-04929113 is an inhibitor of Hsp90 .
PF-04929113 is a water soluble and orally bioavailable prodrug of PF-04928473. It is rapidly absorbed and converted into PF-04928473 after oral administration. In mice bearing BT-474 tumor xenografts, treatment of PF-04928473 causes the degradation of the HER2 client protein. And no obvious toxicity is observed when the dose of PF-04928473 is up to 150mg/kg. Treatment of 100mg/kg PF-04928473 results in complete tumor growth inhibition and in some mice partial tumor regressions. PF-04928473 also shows significant antitumor activity in mice with H1650 xenografts. In addition, as an inhibitor of Hsp90, PF-04928473 is reported to inhibit p-ERK and p-Akt, decrease CD31+ cells and MVD as well as a have an effect on angiogenesis in vivo [1, 2].
 Chandarlapaty S, Sawai A, Ye Q, Scott A, Silinski M, Huang K, Fadden P, Partdrige J, Hall S, Steed P, Norton L, Rosen N, Solit DB. SNX2112, a synthetic heat shock protein 90 inhibitor, has potent antitumor activity against HER kinase-dependent cancers. Clin Cancer Res. 2008 Jan 1;14(1):240-8.
 Okawa Y, Hideshima T, Steed P, Vallet S, Hall S, Huang K, Rice J, Barabasz A, Foley B, Ikeda H, Raje N, Kiziltepe T, Yasui H, Enatsu S, Anderson KC. SNX-2112, a selective Hsp90 inhibitor, potently inhibits tumor cell growth, angiogenesis, and osteoclastogenesis in multiple myeloma and other hematologic tumors by abrogating signaling via Akt and ERK. Blood. 2009 Jan 22;113(4):846-55.