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204001 BX-795 - CAS 702675-74-9 - Calbiochem

204001
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₂₃H₂₆IN₇O₂S702675-74-9

Products

Catalogue NumberPackaging Qty/Pack
204001-10MG Glass bottle 10 mg
Description
OverviewA cell-permeable aminopyrimidine compound that acts as a potent, ATP-competitive and reversible multi-kinase inhibitor (IC50 = 11 nM for PDK1 at ≤ 10 µM of ATP; IC50 = 5 , 6, 19, 31, 41 and 111 nM for NUAK1, TBK1, MARK4, Aurora B, IKKε and PDK1 at 100 µM of ATP, respectively) and displays 50-fold greater selectivity over Cdk2/E, EGFR, GSK-3β, IR, c-Kit, PKA, PKC, TAK1 and VEGFR. Shown to block PDK1/Akt signaling, induce growth arrest and apoptosis in PC-3 and MDA-468 cells (IC50 = 0.25 and 0.75 µM, respectively); further, inhibit phosphorylation (pSer396), nuclear translocation and transcriptional activity of IRF3 and reduce IFN-β production in stimulated macrophages.
Catalogue Number204001
Brand Family Calbiochem®
SynonymsN-(3-((5-Iodo-4-((3-(2-thienylcarbonyl)amino)propyl)amino)-2-pyrimidinyl)amino)phenyl)-1-pyrrolidinecarboxamide, Aurora Kinase Inhibitor VIII, AMPK Related Kinase 5 Inhibitor I, ARK5 Inhibitor I, NUAK Kinase Inhibitor I, NUAK1 Inhibitor I, SnF1 Like Kinase-1 Inhibitor I
References
ReferencesClark, K., et al. 2009. J. Biol. Chem. 284, 14136.
Tamgumcy, T., et al. 2008. Exp. Cell Res. 314, 2299.
Feldman, R.I., et al. 2005. J. Biol. Chem. 280, 19867.
Product Information
CAS number702675-74-9
FormPale yellow solid
Hill FormulaC₂₃H₂₆IN₇O₂S
Chemical formulaC₂₃H₂₆IN₇O₂S
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥95% by HPLC
Physicochemical Information
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
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

Documentation

BX-795 - CAS 702675-74-9 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

BX-795 - CAS 702675-74-9 - Calbiochem Certificates of Analysis

TitleLot Number
204001

References

Reference overview
Clark, K., et al. 2009. J. Biol. Chem. 284, 14136.
Tamgumcy, T., et al. 2008. Exp. Cell Res. 314, 2299.
Feldman, R.I., et al. 2005. J. Biol. Chem. 280, 19867.
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.

Revision15-October-2011 RFH
SynonymsN-(3-((5-Iodo-4-((3-(2-thienylcarbonyl)amino)propyl)amino)-2-pyrimidinyl)amino)phenyl)-1-pyrrolidinecarboxamide, Aurora Kinase Inhibitor VIII, AMPK Related Kinase 5 Inhibitor I, ARK5 Inhibitor I, NUAK Kinase Inhibitor I, NUAK1 Inhibitor I, SnF1 Like Kinase-1 Inhibitor I
DescriptionA cell-permeable aminopyrimidine compound that acts as a potent, ATP-competitive and reversible multi-kinase inhibitor (IC50 = 11 nM for PDK1 at ≤ 10 µM of ATP; IC50 = 5 , 6, 19, 31, 41 and 111 nM for NUAK1, TBK1, MARK4, Aurora B, IKKε and PDK1 at 100 µM of ATP, respectively) and displays 50-fold greater selectivity over Cdk2/E, EGFR, GSK-3β, IR, c-Kit, PKA, PKC, TAK1 and VEGFR. Shown to block PDK1/Akt signaling, induce growth arrest and apoptosis in PC-3 and MDA-468 cells (IC50 = 0.25 and 0.75 µM, respectively); further, inhibit phosphorylation (pSer396), nuclear translocation and transcriptional activity of IRF3 and reduce IFN-β production in stimulated macrophages.
FormPale yellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number702675-74-9
Chemical formulaC₂₃H₂₆IN₇O₂S
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (50 mg/ml)
Storage +2°C to +8°C
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.
Toxicity Standard Handling
ReferencesClark, K., et al. 2009. J. Biol. Chem. 284, 14136.
Tamgumcy, T., et al. 2008. Exp. Cell Res. 314, 2299.
Feldman, R.I., et al. 2005. J. Biol. Chem. 280, 19867.