製品番号: HY-10214

SNX-2112

(別名: PF-04928473)

4 Cited Publications

カスタマーレビュー

Based on 4 publication(s) in Google Scholar

SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a K_d of 16 nM for Hsp90 and IC₅₀s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC₅₀s of 10 nM, 4.275 μM and 0.862 μM, respectively. SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with K_ds of 4 nM, 6 nM and 484 nM, respectively.

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純度: 99.49%
CAS 番号: 908112-43-6
分子式: C₂₃H₂₇F₃N₄O₃
分子量:464.48

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SNX-2112 構造式

CAS 番号: 908112-43-6

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数量

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
化学情報
Publications (4)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a K_d of 16 nM for Hsp90 and IC₅₀s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC₅₀s of 10 nM, 4.275 μM and 0.862 μM, respectively^[1]. SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with K_ds of 4 nM, 6 nM and 484 nM, respectively^[2].

IC₅₀ & Target^[1]

HSP90α

30 nM (IC₅₀)

HSP90β

30 nM (IC₅₀)

GRP94

4275 nM (IC₅₀)

TRAP-1

862 nM (IC₅₀)

HSP アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	1 nM Compound: 9, SNX-2112	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]
A-375	IC₅₀	2 nM Compound: 9, SNX-2112	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	23 nM Compound: 9, SNX-2112	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]
AU565	IC₅₀	10 μM Compound: 9, SNX-2112	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]
AU565	IC₅₀	41 nM Compound: 9, SNX-2112	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]
HCT-15	IC₅₀	52 nM Compound: 9, SNX-2112	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	3 nM Compound: 9, SNX-2112	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]
J774.A1	IC₅₀	<0.06 μM Compound: SNX2112; 1	Cytotoxicity against mouse J774.A1 cells after 72 hrs by MTS assay Cytotoxicity against mouse J774.A1 cells after 72 hrs by MTS assay	[PMID: 28835791]
K562	IC₅₀	6 nM Compound: 9, SNX-2112	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	3 nM Compound: 9, SNX-2112	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	EC₅₀	19 nM Compound: 13b, PF-4928473, SNX-2112	Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2 Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2	[PMID: 22938030]
MCF7	IC₅₀	22 nM Compound: 9, SNX-2112	Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells	[PMID: 20055425]
MCF7	IC₅₀	53 nM Compound: 9, SNX-2112	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	6 nM Compound: 9, SNX-2112	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]
MRC5	CC₅₀	21.34 μM Compound: SNX-2112	Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay	[PMID: 22704890]
NCI-H460	IC₅₀	18 nM Compound: 9, SNX-2112	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	17 nM Compound: 9, SNX-2112	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	6 nM Compound: 9, SNX-2112	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	3 nM Compound: 9, SNX-2112	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]
Vero	CC₅₀	13.33 μM Compound: SNX-2112	Cytotoxicity against african green monkey Vero cells assessed as inhibition of cell viability after 48 hrs by MTT assay Cytotoxicity against african green monkey Vero cells assessed as inhibition of cell viability after 48 hrs by MTT assay	[PMID: 22704890]
Vero	EC₅₀	1.85 μM Compound: SNX-2112	Antiviral activity against HSV2 strain 333 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay Antiviral activity against HSV2 strain 333 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay	[PMID: 22704890]
Vero	EC₅₀	2.26 μM Compound: SNX-2112	Antiviral activity against HSV1 strain F ATCC VR733 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay Antiviral activity against HSV1 strain F ATCC VR733 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay	[PMID: 22704890]

体外実験

SNX-2112 is an orally active Hsp90 inhibitor, with a K_d of 16 nM, and also induces Her-2 degradation, with an IC₅₀ of 10 nM^[3]. SNX-2112 binds to Hsp90, with IC₅₀s of 30 nM, 30 nM, 4.275 μM and 0.862 μM for Hsp90 α and β, Grp94 and Trap-1, respectively^[1]. SNX-2112 shows potent antiproliferative activity against various cancer cell types, with IC₅₀s of 3 nM to 53 nM. SNX-2112 exhibits potent effects on Her2 and p-ERK stability in AU565 cells and p-S6 in A375 cells, with IC₅₀s of 11 ± 5, 41 ± 12, and 1 ± 0.6 nM, respectively. SNX-2112 also induces Hsp70 in A375 cells with an IC₅₀ of 2 ± 0.9 nM^[3]. In addition, SNX-2112 potently blocks signaling of Hsp90 clients, such as Akt, ERK, and NF-κB pathways in different cells. SNX-2112 inhibits multiple myeloma (MM) cell growth, including MM.1S, U266, INA-6, RPMI8226, OPM1, OPM2, MM.1R, and Dox40 MM cell lines, with IC₅₀s of 52, 55, 19, 186, 89, 67, 93, and 53 nM at 48 hours, respectively. SNX-2112 (2.5-10 nM) also suppresses osteoclast formation, associated with down-regulation of ERK/c-fos and PU.1^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

化学情報

CAS 番号 908112-43-6
性状 Solid
分子量 464.48
分子式 C₂₃H₂₇F₃N₄O₃
Color White to off-white
SMILES

FC(F)(C1=NN(C2=CC(N[C@@H]3CC[C@H](CC3)O)=C(C=C2)C(N)=O)C(CC(C)(C4)C)=C1C4=O)F
別名

PF-04928473
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (4)

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Theranostics

Inhibition of HSP90β Improves Lipid Disorders by Promoting Mature SREBPs Degradation via the Ubiquitin-proteasome System. [Abstract]

2019 Aug 12;9(20):5769-5783. PMID: 31534518
Antioxidants (Basel)

A Novel SIRT1 Activator Hydroxygenkwanin Alleviates Osteoporosis by Inhibiting Ferroptosis and Lactylation in Skeletal Stem/Progenitor Cells. [Abstract]

2026 May 12;15(5):612. PMID: 42193234
J Mater Chem B

Suppression of the HSP90-HIF1α pathway with SNX2112-encapsulated nano-micelles for effective triple-negative breast cancer photothermal combined photodynamic therapy. [Abstract]

2025 Jul 2;13(26):7753-7768. PMID: 40468772
J Pharm Biomed Anal

Development and validation of an ultra-performance liquid chromatography-tandem mass spectrometry method for quantification of SR1001, an inverse agonist of retinoid-related orphan receptors, and its application to pharmacokinetic studies in streptozotocin-induced diabetic mice. [Abstract]

2017 Sep 5:143:94-100. PMID: 28578255

溶剤 & 溶解度

体外:

DMSO : 25 mg/mL (53.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1529 mL

10.7647 mL

21.5295 mL

5 mM

0.4306 mL

2.1529 mL

4.3059 mL

10 mM

0.2153 mL

1.0765 mL

2.1529 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

プロトコル

Cell Assay^[4]

To measure proliferation of multiple myeloma (MM) cells and bone marrow stromal cells (BMSCs), the rate of DNA synthesis is measured. MM cells are incubated in 96-well culture plates in the presence of SNX-2112 and/or IL-6 or IGF-1 or BMSCs for 48 hours. Cells are pulsed with 0.5 μCi/well of [³H]-thymidine during the last 8 hours of culture, harvested onto glass filters with an automatic cell harvester, and counted using the LKB Betaplate scintillation counter. Inhibition of proliferation by test compounds (SNX-2112) in solid tumor cell lines is measured in 96-well plates after 72 hours of treatment with Cyquant DNA binding dye. AML, LCL, and K562 cell line proliferation rates are measured after 72 hours of compound treatment with CellTiter-Glo^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
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RP-HPLC (2659 KB)
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MS (2659 KB)
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IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. 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]

[2]. Mishra SJ, et al. Transformation of the Non-Selective Aminocyclohexanol-Based Hsp90 Inhibitor into a Grp94-Seletive Scaffold. ACS Chem Biol. 2017 Jan 20;12(1):244-253. [Content Brief]

[3]. 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]

[4]. Okawa Y, et al. SNX-2112, a selective Hsp90 inhibitor, potently inhibits tumor cell growth, angiogenesis, and osteoclastogenesis in multiple myeloma and other hematologic tumors by abrogating signaling via Akt and ERK. Blood. 2009 Jan 22;113(4):846-55. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1529 mL	10.7647 mL	21.5295 mL	53.8236 mL
	5 mM	0.4306 mL	2.1529 mL	4.3059 mL	10.7647 mL
	10 mM	0.2153 mL	1.0765 mL	2.1529 mL	5.3824 mL
	15 mM	0.1435 mL	0.7176 mL	1.4353 mL	3.5882 mL
	20 mM	0.1076 mL	0.5382 mL	1.0765 mL	2.6912 mL
	25 mM	0.0861 mL	0.4306 mL	0.8612 mL	2.1529 mL
	30 mM	0.0718 mL	0.3588 mL	0.7176 mL	1.7941 mL
	40 mM	0.0538 mL	0.2691 mL	0.5382 mL	1.3456 mL
	50 mM	0.0431 mL	0.2153 mL	0.4306 mL	1.0765 mL

Keywords

SNX-2112

4 Cited Publications

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SNX-2112

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Anti-Blood Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cuproptosis Compound Library

Cancer Stem Cells Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Extracellular Vesicles (EVs) Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

MedChemExpress（MCE）の使用を引用している文献 SNX-2112

HSP アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (4)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

SNX-2112

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Anti-Blood Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cuproptosis Compound Library

Cancer Stem Cells Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Extracellular Vesicles (EVs) Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

MedChemExpress（MCE）の使用を引用している文献 SNX-2112

HSP アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (4)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

SNX-2112 関連分類

HY-10214 関連分類