SNX-5422 mesylate
Based on 1 publication(s) in Google Scholar
SNX-5422 Mesylate (PF-04929113 Mesylate), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37 nM.
For research use only. We do not sell to patients.
- CAS No.: 1173111-67-5
- Formula: C26H34F3N5O7S
- Molecular Weight:617.64
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) SNX-5422 mesylate
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Biological Activity
Description
IC50 & Target
[1]|
HSP90 41 nM (Kd) |
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
13 nM
Compound: 10, SNX-5422
|
Inhibition of Hsp90 in human A375 cells assessed as Hsp70 induction after 24 hrs by high content screening
Inhibition of Hsp90 in human A375 cells assessed as Hsp70 induction after 24 hrs by high content screening
|
[PMID: 19552433] |
| A-375 | IC50 |
51 nM
Compound: 10, SNX-5422
|
Antiproliferative activity against human A375 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human A375 cells after 72 to 144 hrs by cyquant DNA dye method
|
[PMID: 19552433] |
| A-375 | IC50 |
61 nM
Compound: 10, SNX-5422
|
Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening
Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening
|
[PMID: 19552433] |
| AU565 | IC50 |
11 nM
Compound: 10, SNX-5422
|
Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening
Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening
|
[PMID: 19552433] |
| AU565 | IC50 |
5 μM
Compound: 10, SNX-5422
|
Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening
Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening
|
[PMID: 19552433] |
| HCT-15 | IC50 |
190 nM
Compound: 10, SNX-5422
|
Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method
|
[PMID: 19552433] |
| HT-29 | IC50 |
32 nM
Compound: 10, SNX-5422
|
Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method
|
[PMID: 19552433] |
| K562 | IC50 |
23 nM
Compound: 10, SNX-5422
|
Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method
|
[PMID: 19552433] |
| LNCaP | IC50 |
31 nM
Compound: 10, SNX-5422
|
Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method
|
[PMID: 19552433] |
| MCF7 | IC50 |
16 nM
Compound: 10, SNX-5422
|
Antiproliferative activity against human MCF7 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human MCF7 cells after 72 to 144 hrs by cyquant DNA dye method
|
[PMID: 19552433] |
| MDA-MB-231 | IC50 |
38 nM
Compound: 10, SNX-5422
|
Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method
|
[PMID: 19552433] |
| NCI-H460 | IC50 |
215 nM
Compound: 10, SNX-5422
|
Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method
|
[PMID: 19552433] |
| PC-3 | IC50 |
114 nM
Compound: 10, SNX-5422
|
Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method
|
[PMID: 19552433] |
| SK-MEL-5 | IC50 |
25 nM
Compound: 10, SNX-5422
|
Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method
|
[PMID: 19552433] |
| SW-620 | IC50 |
19 nM
Compound: 10, SNX-5422
|
Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method
|
[PMID: 19552433] |
In Vitro
SNX-5422 is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37 nM. SNX-5422 exhibits potent effects on Her2 and p-ERK stability in AU565 cells and p-S6 in A375 cells, with IC50s of 5 ± 1, 11 ± 3, and 61 ± 22 nM, respectively. SNX-5422 also induces Hsp70 in A375 cells with an IC50 of 13 ± 3 nM[1]. SNX-5422 (SNX5422; 0.5, 1, 2, 5, and 10 μM) reduces cell viability in a concentration-dependent manner. Moreover, SNX-5422 (1, 3, 5, 7 μM) in combination with equal amounts of HDAC inhibitors (PXD101, SAHA, and TSA) synergistically induces cell death via suppression of PI3K/Akt/mTOR signaling in ATC cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1173111-67-5
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Molecular Weight 617.64
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Formula C26H34F3N5O7S
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SMILES
CS(=O)(O)=O.O=C1CC(C)(C)CC2=C1C(C(F)(F)F)=NN2C3=CC=C(C(N[C@@H]4CC[C@@H](OC(CN)=O)CC4)=C3)C(N)=O
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Synonyms
PF-04929113 mesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
-
Most Recent
Purity & Documentation
References
[1]. Huang KH, et al. Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. J Med Chem. 2009 Jul 23;52(14):4288-305 [Content Brief]
[2]. Chandarlapaty S, et al. 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. [Content Brief]
[3]. Kim SH, et al. The heat shock protein 90 inhibitor SNX5422 has a synergistic activity with histone deacetylase inhibitors in induction of death of anaplastic thyroid carcinoma cells. Endocrine. 2016 Feb;51(2):274-82. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)