Molecular Weight(MW): 521.53
PF-04929113 (SNX-5422) is a potent and selective HSP90 inhibitor with Kd of 41 nM and induces Her-2 degradation with IC50 of 37 nM. Phase 1/2.
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Effect of SNX-2112 on E. histolytica morphology. Trophozoites were treated with 3 uM SNX-2112 for 48 h. (A) E. histolytica trophozoites treated with 0.5% DMSO. Arrow indicates live trophozoite. Magnification, x 10. (B) E. histolytica trophozoites treated with 3 uM SNX-2112. Treatment caused complete lysis of trophozoites (arrow). Magnification, x 10. Trophozoites were imaged under phase-contrast microscope.
Antimicrob Agents Chemother 2014 58(7), 4138-44. PF-04929113 (SNX-5422) purchased from Selleck.
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|Description||PF-04929113 (SNX-5422) is a potent and selective HSP90 inhibitor with Kd of 41 nM and induces Her-2 degradation with IC50 of 37 nM. Phase 1/2.|
PF-04929113 is a small-molecule Hsp90 inhibitor based on the 6,7-dihydro-indazol-4-one scaffold. PF-04929113 developed by Serenex, converts to SNX-2122, which is the active Hsp90 inhibitor form. PF-04929113 exhibits potent effects on Her-2 stability and causes expected up-regulation of Hsp70. PF-04929113 shows potent antiproliferative activity against a broad range of cancer cell types, e.g. MCF-7 (IC50=16 nM), SW620 (IC50=19 nM), K562 (IC50=23 nM), SK-MEL-5 (IC50=25 nM), and A375 (IC50=51 nM). 
|In vivo||PF-04929113 inhibits human MM cell growth in vivo, and immuno-histochemical analysis shows PF-04929113 significantly inhibits p-ERK and p-Akt in treated mice. Meanwhile, PF-04929113 treatment significantly decreases the percentage of CD31+ cells and MVD, consistent with an inhibitory effect on angiogenesis in vivo. A 50 mg/kg administration of PF-04929113 delivered 3 times per week significantly delays castrate-resistant LNCaP tumor growth and prolongs cancer specific survival.  Immuno-histochemical analysis indicates increased SP70 expression, and decreases Ki67, Akt, and AR expression, after treatment with PF-04929113. Inhibition of tumor progression by PF-04929113 may result from a combination of decreased proliferative (reduced Ki67 and Akt expression) or increased apoptosis (increased ApopTag staining) rates. |
Affinity for Hsp90:Hsp90 from porcine spleen extract is isolated by affinity capture on a purine-affinity media. The Hsp90 loaded media is then challenged with PF-04929113 at a given concentration, ranging from 0.8 to 500 μM, and the amount of Hsp90 liberated at each concentration is determined by Bradford protein assay. The resulting IC50 values are corrected for the ATP ligand concentration and presented as apparent Kd values.
|In vitro||DMSO||104 mg/mL (199.41 mM)|
|Ethanol||5 mg/mL (9.58 mM)|
|In vivo||0.5% CMC+0.25% Tween 80||25 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02612285||Recruiting||Cancer||Esanex Inc.||March 2016||Phase 2|
|NCT02063958||Active, not recruiting||Cancer||Esanex Inc.||February 2014||Phase 1|
|NCT01635712||Active, not recruiting||Cancer||Esanex Inc.||February 2014||Phase 1|
|NCT01892046||Active, not recruiting||Cancer||Esanex Inc.||November 2013||Phase 1|
|NCT01848756||Terminated||Cancer||Esanex Inc.||April 2013||Phase 1|Phase 2|
|NCT01851096||Active, not recruiting||Cancer||Esanex Inc.||March 2013||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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