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SNX2112

Catalog No. T6305 CAS 908112-43-6

Synonyms: SNX-2112, PF 04928473, SNX 2112

SNX2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

SNX2112, CAS 908112-43-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 68.00
2 mg	In stock	$ 98.00
5 mg	In stock	$ 167.00
10 mg	In stock	$ 227.00
25 mg	In stock	$ 387.00
50 mg	In stock	$ 587.00
100 mg	In stock	$ 839.00
500 mg	In stock	$ 1,720.00
1 mL * 10 mM (in DMSO)	In stock	$ 183.00

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Purity: 99.95%

Purity: 99.46%

Purity: 98.93%

Purity: 98.9%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SNX2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM.
Targets&IC50	HSP90 β:30 nM(Ka), HSP90 α:30 nM(Ka)
In vitro	Treatment of BT-474 cells with 1 μM SNX-2112 results in down-regulation of HER2 expression within 3 to 6 hours of drug exposure with near-complete loss of HER2 expression by 10 hours. Treatment with SNX-2112 also results in a decline in total Akt expression. SNX-2112 inhibits cell proliferation with IC50 values ranging from 10 to 50 nM, in BT474, SKBR-3, SKOV-3, MDA-468, MCF-7 and H1650 cancer cells. And these antiproliferative effects are associated with hypophosphorylation of Rb, arrest of G1 and modest levels of apotosis. [1] SNX-2112 competitively binds to the N-terminal adenosine triphosphate binding site of Hsp90. SNX-2112 induces apoptosis via caspase-8, -9, -3, and poly (ADPribose) polymerase cleavage. SNX-2112 inhibits cytokine-inducedAkt and extracellular signal-related kinase (ERK) activation and also overcomes the growth advantages conferred by interleukin-6, insulin-like growth factor-1, and bone marrow stromal cells. SNX-2112 inhibits tube formation by human umbilical vein endothelial cells via abrogation of eNOS/Akt pathway and markedly inhibits osteoclast formation via down-regulation of ERK/c-fos and PU.1. [2] Cell lines (eight cell lines from osteosarcoma, neuroblastoma, hepatoblastoma, and ymphoma) studied demonstrates sensitivity to SNX-2112 with IC50 values ranging from 10-100?nM. A higher dose (70?nM) exhibits a more prolonged inhibition and larger sub-G1 accumulation. Observed levels of Akt1 and C-Raf are markedly reduced over time along with an increase in PARP cleavage. [3] A recent research indicates NX-2112 induces autophagy in a time- and dose-dependent manner via Akt/mTOR/p70S6K inhibition. SNX-2112 induces significant apoptosis and utophagy in human melanoma A-375 cells, and may be an effective targeted therapy agent. [4]
In 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. [2]
Kinase Assay	ATP Displacement Assay: For the protein affinity-displacement assay, a purine-based affinity resin is generated by incubating ATP-linked Sepharose with Jurkat cell lysate (flash frozen and homogenized in saline) at 4 °C. This is then incubated with SNX-2112 for 90 minutes. Proteins eluted by drug are then resolved by SDS-PAGE, visualized with silver staining, and excised from the gel for MS-based identification. Briefly, after destaining and trypsin digestion, peptides are extracted with μC18 ZipTips and then eluted and spotted directly to a conventional stainless steel matrix-assisted laser desorption/ionization target with a saturated solution of α-cyano-4- hydroxycinnamic acid in 50% acetonitrile, 0.15% formic acid. Mass spectra are then acquired using a MALDI-TOF/TOF 4700 Proteomics Analyzer. MS spectra are acquired (1,000 shots per spectrum), and the three peaks from each with the greatest signal-to-noise ratio are automatically submitted for tandem MS analysis (3000 shots per spectrum). The collision energy is 1keV. Air is used as the collision gas. Protein identification is done from the MS and tandem MS data using GPS Explorer software with the integrated Mascot database search engine.
Cell Research	Cell viability is determined by seeding 2-5 × 103 cells per well in 96- well plates and treating with SNX-2112 24 hours after plating in complete medium (200 μL). Each drug concentration is tested in eight wells. Cells are assayed using the Alamar blue viability test after a 96-h incubation. Flow cytometry is done using nuclei stained with ethidium bromide and isolated via the Nusse protocol(Only for Reference)

Synonyms	SNX-2112, PF 04928473, SNX 2112
Molecular Weight	464.48
Formula	C23H27F3N4O3
CAS No.	908112-43-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 1 mg/mL (2.15 mM)

DMSO: 86 mg/mL (185.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Chandarlapaty S, et al, Clin Cancer Res, 2008, 14(1), 240-248. 2. Okawa Y, et al, Blood, 2009, 113(4), 846-855. 3. Chinn DC, et al, Pediatr Blood Cancer, 2012, 58(6), 885-890. 4. Liu KS, et al, Cancer Lett, 2012, 318(2), 180-188.

Citations

1. Zhao D, Xu Y M, Cao L Q, et al. Complex Crystal Structure Determination and in vitro Anti–non–small Cell Lung Cancer Activity of Hsp90N Inhibitor SNX-2112. Frontiers in cell and developmental biology. 2021, 9: 567. 2. Zhao D, Xu Y M, Cao L Q, et al. Complex Crystal Structure Determination and in vitro Anti–non–small Cell Lung Cancer Activity of Hsp90N Inhibitor SNX-2112. Frontiers in cell and developmental biology. 2021, 9: 567.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Preclinical Compound Library Hematonosis Compound Library HIF-1 Signaling Pathway Compound Library Endoplasmic Reticulum Stress Compound Library Apoptosis Compound Library Cytoskeletal Signaling Pathway Compound Library Metabolism Compound Library Anti-Metabolism Disease Compound Library

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

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SNX2112 908112-43-6 Cytoskeletal Signaling Metabolism HSP PF04928473 SNX-2112 PF-04928473 PF 04928473 SNX 2112 inhibitor inhibit

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