SNX-2112 (PF-04928473)

Alias: PF 04928473; SNX2112; SNX-2112;PF-04928473; PF04928473; SNX 2112
Cat No.:V0888 Purity: ≥98%
SNX-2112 (SNX2112; SNX 2112;PF-04928473; PF04928473)is a novel and potent HSP90(Heat Shock Protein 90) with potential antitumor activity and was inphase 1 clinical trials.
SNX-2112 (PF-04928473) Chemical Structure CAS No.: 908112-43-6
Product category: HSP
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

SNX-2112 (SNX2112; SNX 2112; PF-04928473; PF04928473) is a novel and potent HSP90 (Heat Shock Protein 90) with potential antitumor activity and was in phase 1 clinical trials. It selectively inhibits HSP90α and HSP90β with Ka values of 30 nM and 30 nM. It exhibits excellent in vivo antitumor efficacy in in a xenograft murine model.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
SNX-2112 is an oral active Hsp90 inhibitor that has an IC50 of 10 nM and a Kd of 16 nM for Her-2 degradation[3]. SNX-2112 binds to Hsp90; its IC50 values for Hsp90 α and β, Grp94, and Trap-1 are 30 nM, 30 nM, 4.275 μM, and 0.862 μM, respectively [1]. IC50 values for SNX-2112 range from 3 nM to 53 nM, indicating strong antiproliferative action against several types of cancer cells. With IC50 values of 11 ± 5, 41 ± 12, and 1 ± 0.6 nM, respectively, SNX-2112 exhibited strong impacts on Her2 and p-ERK stability in AU565 cells and p-S6 in A375 cells. With an IC50 of 2 ± 0.9 nM, SNX-2112 also activates Hsp70 in A375 cells[3]. Furthermore, Hsp90 client signaling, including the Akt, ERK, and NF-κB pathways, can be efficiently blocked in many cell types by SNX-2112. With IC50 values of 52, 55, 19, 186, 89, 67, 93, and 53 nM at 48 hours, SNX-2112 suppresses the proliferation of multiple myeloma (MM) cell lines, including MM.1S, U266, INA-6, RPMI8226, OPM1, OPM2, MM.1R, and Dox40 MM cell lines. Along with downregulating ERK/c-fos and PU.1, SNX-2112 (2.5–10 nM) also prevents the development of osteoclasts [4].
ln Vivo
SNX-2112, delivered by its prodrug SNX-5422, inhibits MM cell growth and prolongs survival in a xenograft murine model and blockade of Hsp90 by SNX-2112 not only inhibits MM cell growth but also acts in the bone marrow microenvironment to block angiogenesis and osteoclastogenesis.
Animal Protocol
Dissolved in 1% carboxy methylcellulose/0.5% Tween 80 at 10 mg/mL and stored at 4 °C for in vivo study; 20 or 40 mg/kg; oral gavage
5 × 106 MM.1S cells are inoculated subcutaneously in the Fox Chase SCID mice
References
[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.
[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.
[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
[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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H27F3N4O3
Molecular Weight
464.48
CAS #
908112-43-6
SMILES
O=C(N)C1=CC=C(N2N=C(C(F)(F)F)C3=C2CC(C)(C)CC3=O)C=C1N[C@H]4CC[C@H](O)CC4
InChi Key
ZFVRYNYOPQZKDG-MQMHXKEQSA-N
InChi Code
InChI=1S/C23H27F3N4O3/c1-22(2)10-17-19(18(32)11-22)20(23(24,25)26)29-30(17)13-5-8-15(21(27)33)16(9-13)28-12-3-6-14(31)7-4-12/h5,8-9,12,14,28,31H,3-4,6-7,10-11H2,1-2H3,(H2,27,33)/t12-,14-
Chemical Name
4-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl)-2-(((1r,4r)-4-hydroxycyclohexyl)amino)benzamide
Synonyms
PF 04928473; SNX2112; SNX-2112;PF-04928473; PF04928473; SNX 2112
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 93 mg/mL (200.2 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
0.5% CMC+0.25% Tween 80: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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
10 mM 0.2153 mL 1.0765 mL 2.1529 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
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