Molecular structure of PF-04929113, CAS Number: 908115-27-5
PF-04929113 (CAS 908115-27-5)
Alternate Names:
SNX-5422; (1r,4r)-4-(2-carbamoyl-5-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydroindazol-1-yl)phenylamino)cyclohexyl 2-aminoacetate
Application:
PF-04929113 is a potent and selective inhibitor of Hsp90 and of Her-2 degradation
CAS Number:
908115-27-5
Purity:
≥98%
Molecular Weight:
521.53
Molecular Formula:
C25H30F3N5O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
PF-04929113 (SNX-5422) is a potent and selective Hsp90 inhibitor (Kd of 41 nM). PF-04929113 also inhibits Her-2 degradation (IC50 of 37 nM). PF-04929113 is a small-molecule Hsp90 inhibitor based on the 6,7-dihydro-indazol-4-one scaffold. 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 of 19 nM), K562 (IC50 of 23 nM), SK-MEL-5 (IC50 of 25 nM), and A375 (IC50 of 51 nM).
PF-04929113 (CAS 908115-27-5) References
- Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. | Huang, KH., et al. 2009. J Med Chem. 52: 4288-305. PMID: 19552433
- Determination of PF-04928473 in human plasma using liquid chromatography with tandem mass spectrometry. | Jain, L., et al. 2010. J Chromatogr B Analyt Technol Biomed Life Sci. 878: 3187-92. PMID: 20951100
- A novel HSP90 inhibitor delays castrate-resistant prostate cancer without altering serum PSA levels and inhibits osteoclastogenesis. | Lamoureux, F., et al. 2011. Clin Cancer Res. 17: 2301-13. PMID: 21349995
- Clusterin inhibition using OGX-011 synergistically enhances Hsp90 inhibitor activity by suppressing the heat shock response in castrate-resistant prostate cancer. | Lamoureux, F., et al. 2011. Cancer Res. 71: 5838-49. PMID: 21737488
- A phase I study of PF-04929113 (SNX-5422), an orally bioavailable heat shock protein 90 inhibitor, in patients with refractory solid tumor malignancies and lymphomas. | Rajan, A., et al. 2011. Clin Cancer Res. 17: 6831-9. PMID: 21908572
- Phase I trial of the HSP90 inhibitor PF-04929113 (SNX5422) in adult patients with recurrent, refractory hematologic malignancies. | Reddy, N., et al. 2013. Clin Lymphoma Myeloma Leuk. 13: 385-91. PMID: 23763921
- Suppression of heat shock protein 27 using OGX-427 induces endoplasmic reticulum stress and potentiates heat shock protein 90 inhibitors to delay castrate-resistant prostate cancer. | Lamoureux, F., et al. 2014. Eur Urol. 66: 145-55. PMID: 24411988
- Targeting heat shock proteins in metastatic castration-resistant prostate cancer. | Azad, AA., et al. 2015. Nat Rev Urol. 12: 26-36. PMID: 25512207
- Mild microwave ablation combined with HSP90 and TGF‑β1 inhibitors enhances the therapeutic effect on osteosarcoma. | Chen, L., et al. 2020. Mol Med Rep. 22: 906-914. PMID: 32468060
- High-throughput screening as a drug repurposing strategy for poor outcome subgroups of pediatric B-cell precursor Acute Lymphoblastic Leukemia. | Oikonomou, A., et al. 2023. Biochem Pharmacol. 217: 115809. PMID: 37717691
Inhibitor of:
DEME-6, FKBP52, HSP, IKK-i, LDLRAD1, and SGT1.Activator of:
HSP 78.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PF-04929113, 5 mg | sc-364576 | 5 mg | $495.00 | |||
PF-04929113, 50 mg | sc-364576A | 50 mg | $1980.00 |