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SNX-2112

Cat. No. M3528
SNX-2112 Structure
Synonym:

PF-04928473

Size Price Availability
5mg USD 245 Out of stock
10mg USD 330 Out of stock
50mg USD 850 Out of stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

SNX-2112 is a potent synthetic heat shock protein 90 inhibitor with an IC50 of 0.92 μM for K562 cells. The heat shock protein 90 (Hsp90) chaperone not only regulates the conformational maturation but also stables the structures of oncogenic kinases as well as transcription factors. SNX-2112 is an active metabolite of the compounds SNX-5542. SNX-2112 is rapidly transformed form SNX-5542 after administration. In a panel of tumor cell lines, SNX-2112 degraded HER2 and mutant epidermal growth factor receptor and inhibited extracellular signal-modulated kinase and Akt activation.SNX-2112 inducen a Rb-dependent G1 arrest with subsequent apoptosis. which accumulates in tumors relative to normal tissues.

Protocol
Cell Experiment
Cell lines BT474, SKBR-3, SKOV-3, MDA-468, MCF-7 and H1650 cancer cells
Preparation method Determining cell viability 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). Testing each drug concentration in eight wells. After a 96-h incubation ,using the Alamar blue viability test to assay cells . Flow cytometry is done using nuclei stained with ethidium bromide and isolated via the Nusse protocol
Concentrations 0-500 nM
Incubation time 24 hours
Animal Experiment
Animal models 5 ?106 MM.1S cells are inoculated subcutaneously in the Fox Chase SCID mice (6-7 weeks old).
Formulation SNX-5422 is dissolved in 1% carboxy methylcellulose/0.5% Tween 80 at 10 mg/mL and stored at 4 癈 for in vivo stud
Dosages 20 or 40 mg/kg
Administration SNX-5422 is administered orally 3 times per week, total 3 weeks.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 464.48
Formula C23H27F3N4O3
CAS Number 908112-43-6
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SNX-2112, PF-04928473 supplier, HSP90, inhibitors

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