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533379 p21-Activated Kinase Inhibitor III, FRAX597 - CAS 1286739-19-2 - Calbiochem

533379
  
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1286739-19-2C₂₉H₂₈ClN₇OS
Description
Overview

This product has been discontinued.



A cell-permeable, orally bioavailable, pyridopyrimidinone compound that acts as a potent, reversible, and ATP-competitive isoforms selective inhibitor of p21 activated kinase (PAK; IC50 = 7.7, 12.8, and 19.3 nM for PAK1, 2, and 3, respectively). Binds to the back cavity of the ATP binding site of PAK1, and exhibits much reduced activity towards V342F and V342Y mutant forms of PAK1 (IC50 = 3 and 2 µM, respectively). Does not affect the activity of PAK4, 6, and 7 (IC50 > 10 µM). At higher concentrations (100 nM), is shown to cause over 80% inhibition of YES1, RET, CSF1R, and TEK. Reported to block the proliferation of schwannoma cell proliferation by blocking cell cycle at G1 phase. Also blocks the neurofibromatosis 2 (NF2)-associated tumor growth in mice (100 mg/kg, oral for 14 days).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Catalogue Number533379
Brand Family Calbiochem®
Synonyms6-(2-Chloro-4-(thiazol-5-yl)phenyl)-8-ethyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrido[2,3-d]pyrimidin-7(8H)-one, PAK Inhibitor III, FRAX-597
References
ReferencesLicciulli, S., et al. 2013. J. Biol. Chem. 288, 29105.
Chow, H.Y., et al. 2012. Cancer Res. 72, 5966.
Product Information
CAS number1286739-19-2
FormOff-white solid
Hill FormulaC₂₉H₂₈ClN₇OS
Chemical formulaC₂₉H₂₈ClN₇OS
Hygroscopic Hygroscopic
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary Targetp21 activated kinase
Primary Target IC<sub>50</sub>7.7, 12.8, and 19.3 nM for PAK1, 2, and 3, respectively
Purity≥97% 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 +2°C to +8°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
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
533379 0

Documentation

p21-Activated Kinase Inhibitor III, FRAX597 - CAS 1286739-19-2 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Licciulli, S., et al. 2013. J. Biol. Chem. 288, 29105.
Chow, H.Y., et al. 2012. Cancer Res. 72, 5966.
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.

Revision20-November-2015 JSW
Synonyms6-(2-Chloro-4-(thiazol-5-yl)phenyl)-8-ethyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrido[2,3-d]pyrimidin-7(8H)-one, PAK Inhibitor III, FRAX-597
DescriptionA cell-permeable, orally bioavailable, pyridopyrimidinone compound that acts as a potent, reversible, and ATP-competitive isoforms selective inhibitor of p21 activated kinase (PAK; IC50 = 7.7, 12.8, and 19.3 nM for PAK1, 2, and 3, respectively). Binds to the back cavity of the ATP binding site of PAK1, and exhibits much reduced activity towards V342F and V342Y mutant forms of PAK1 (IC50 = 3 and 2 µM, respectively). Does not affect the activity of PAK4, 6, and 7 (IC50 > 10 µM). At higher concentrations (100 nM), is shown to cause over 80% inhibition of YES1, RET, CSF1R, and TEK. Reported to block the proliferation of schwannoma cell proliferation by blocking cell cycle at G1 phase. Also blocks the neurofibromatosis 2 (NF2)-associated tumor growth in mice (100 mg/kg, oral for 14 days).
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1286739-19-2
Chemical formulaC₂₉H₂₈ClN₇OS
Purity≥97% by HPLC
SolubilityDMSO (10 mg/ml)
Storage Protect from light
+2°C to +8°C
Hygroscopic
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
ReferencesLicciulli, S., et al. 2013. J. Biol. Chem. 288, 29105.
Chow, H.Y., et al. 2012. Cancer Res. 72, 5966.