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504045 Focal Adhesion Kinase Inhibitor III - CAS 1426683-53-5 - Calbiochem

504045
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1426683-53-5C₂₂H₂₆N₄O₂S

Products

Catalogue NumberPackaging Qty/Pack
5.04045.0001 Sklená flaša 10 mg
Description
OverviewA cell-permeable pyrazolobenzothiazinedioxide compound that targets and locks FAK in its inactive conformation, resulting in preincubation time-dependent inhibition in kinase assays and FAK autophosphorylation in human prostate cancer PC3M-luc cells (IC50 = 7.1 µM with 30 min inhibitor preincubation), while exhibiting little activity toward Akt1, Aurora B, HER2, MEK1, p38α, Pyk2, or Src even at concentrations as high as 10 µM.
Catalogue Number504045
Brand Family Calbiochem®
SynonymsFAK Inhibitor III, N-(4-tert-Butylbenzyl)-1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine-4,4-dioxide
References
ReferencesTomita, N., et al. 2013. Bioorg. Med. Chem. Lett. 23, 1779.
Product Information
CAS number1426683-53-5
FormOff-white powder
Hill FormulaC₂₂H₂₆N₄O₂S
Chemical formulaC₂₂H₂₆N₄O₂S
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetFAK
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
5.04045.0001 04055977264272

Documentation

Focal Adhesion Kinase Inhibitor III - CAS 1426683-53-5 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Tomita, N., et al. 2013. Bioorg. Med. Chem. Lett. 23, 1779.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision17-July-2013 JSW
SynonymsFAK Inhibitor III, N-(4-tert-Butylbenzyl)-1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine-4,4-dioxide
DescriptionA cell-permeable pyrazolobenzothiazinedioxide compound that targets and locks FAK in its inactive conformation, resulting in preincubation time-dependent inhibition against FAK kinase activity in cell-free assays (IC50 = 0.64 and 2.2 µM, respectively, with 60 or 5 min FAK-inhibitor preincubation before substrate poly-GT and 0.5 µM ATP addition) and FAK autophosphorylation in human prostate cancer PC3M-luc cells (IC50 = 7.1 µM with 30 min inhibitor preincubation before 2 h stimulation by plating cells on fibronectin-coated surface), while exhibiting little activity toward Akt1, Aurora B, HER2, MEK1, p38α, Pyk2, or Src even at concentrations as high as 10 µM.
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1426683-53-5
Chemical formulaC₂₂H₂₆N₄O₂S
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesTomita, N., et al. 2013. Bioorg. Med. Chem. Lett. 23, 1779.