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
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) SNX-5422 mesylate
More
Biological Activity
|
HSP90 41 nM (Kd) |
|
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] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1173111-67-5
-
Molecular Weight 617.64
-
Formula C26H34F3N5O7S
-
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
-
Synonyms
PF-04929113 mesylate
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
-
Journal Impact Factor
-
Most Recent
Protocol
Briefly, Hsp90 from porcine spleen extract is isolated by affinity capture on a purine-affinity media. The Hsp90 loaded media is then challenged with test compound (SNX-5422) at a given concentration, ranging from 0.8 to 500 μM, and the amount of Hsp90 liberated at each concentration is determined. The resulting IC50 values are corrected for the ATP ligand concentration and presented as apparent Kd values[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell viability is determined by the CCK-8 Assay Kit. Cells (5 × 103/100 μL) in each well on 96-well plates are incubated overnight, and treated with the drugs (SNX-5422) for an additional 4 h at 37°C. Absorbance is measured at 450 nm using a spectrophotometer. All experiments are performed in triplicate[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Female nude mice are 11 to 12 weeks old and have a body weight range of 18.7−30.5 g on Day 1 of the study. Xenografts are initiated from HT-29 human colon carcinoma tumors maintained by serial transplantation in athymic nude mice. Each test mouse receives a 1 mm3 HT-29 tumor fragment implanted subcutaneously in the right flank, and the growth of tumors is monitored as the average size approached 80−120 mm3. Fourteen days later, designated as Day 1 of the study, individual tumor volumes range from 63 to 126 mm3 and the animals are placed into eight groups, each consisting of 10 mice with group mean tumor volumes of 93.2−93.9 mm3. Micronized SNX-5422 is preformulated in 1% microcrystalline cellulose/0.5% Tween80 in water. The solutions are stored at 4°C during the study and homogenized just prior to dosing. Group 1 vehicle control mice receive D5W (5% dextrose) vehicle by oral gavage beginning on Day 1, every other day for three doses, followed by two days without treatment, for three cycles ((qod × 3)/2 × 3 weeks, total of nine doses). Groups 2 to 5 animals receive 10 at 5, 10, 25, or 50 mg/kg on the same schedule as vehicle control group ((qod × 3)/2 × 3). Each treatment is administered in a volume of 0.2 mL per 20 g of body weight (10 mL/kg) and is scaled to the body weight of the animal. Tumors are measured twice weekly using calipers[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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)
SNX-5422 mesylate Related Classifications
HY-10213A Related Classifications
Powered by Bioz