2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Autophagy
  3. HSP Autophagy
  4. SNX-2112

SNX-2112  (Synonyms: PF-04928473)

Cat. No.: HY-10214 Purity: 99.41%
COA Handling Instructions

Molarity Calculator

SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd 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 Kds of 4 nM, 6 nM and 484 nM, respectively.

For research use only. We do not sell to patients.

SNX-2112 Chemical Structure

SNX-2112 Chemical Structure

CAS No. : 908112-43-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 92 In-stock
Solution
10 mM * 1 mL in DMSO USD 92 In-stock
Solid
1 mg USD 36 In-stock
5 mg USD 90 In-stock
10 mg USD 150 In-stock
50 mg USD 450 In-stock
100 mg USD 750 In-stock
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Based on 2 publication(s) in Google Scholar

SNX-2112 Related Antibodies

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View All HSP Isoform Specific Products:

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd 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 Kds 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)

In Vitro

SNX-2112 is an orally active Hsp90 inhibitor, with a Kd 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.

SNX-2112 Related Antibodies
Molecular Weight

464.48

Formula

C23H27F3N4O3
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1529 mL 10.7647 mL 21.5295 mL
5 mM 0.4306 mL 2.1529 mL 4.3059 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.41%

COA (256 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References
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].

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

Complete Stock Solution Preparation Table

* 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.

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
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SNX-2112 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SNX-2112908112-43-6PF-04928473SNX2112SNX 2112PF04928473PF 04928473HSPAutophagyHeat shock proteinsInhibitorinhibitorinhibit

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