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.
8505C and CAL62 cells were treated with SNX5422 at 5 μM for 72 h, and the protein levels of hsp90, hsp70, Raf-1, GSK3b, and total and phospho-Akt were measured. All experiments were performed in triplicate. The blots are representative of independent experiments.
Endocrine, 2016, 51(2):274-82.. PF-04929113 (SNX-5422) purchased from Selleck.
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4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|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|
|NCT02973399||Recruiting||Cancer||Esanex Inc.||February 7, 2017||Phase 1|
|NCT00644072||Completed||Lymphoma|Neoplasms||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||March 7, 2008||Phase 1|
|NCT02612285||Terminated||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|
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