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1439934-41-4

1439934-41-4 structure
1439934-41-4 structure
  • Name: CTX0294885
  • Chemical Name: 2-((5-chloro-2-((4-(piperazin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)-N-methylbenzamide
  • CAS Number: 1439934-41-4
  • Molecular Formula: C22H24ClN7O
  • Molecular Weight: 437.925
  • Catalog: Chemical reagent Organic reagent Amide
  • Create Date: 2018-03-26 05:59:51
  • Modify Date: 2024-01-02 13:32:32
  • CTX-0294885 is a a novel bisanilino pyrimidine; exhibits inhibitory activity against a broad range of kinases in vitro, and further developed it into a Sepharose-supported kinase capture reagent.Target: Kinase capture reagentUse of a quantitative proteomics approach confirmed the selectivity of CTx-0294885-bound beads for kinase enrichment. Large-scale CTx-0294885-based affinity purification followed by LC-MS/MS led to the identification of 235 protein kinases from MDA-MB-231 cells, including all members of the AKT family that had not been previously detected by other broad-spectrum kinase inhibitors. Addition of CTx-0294885 to a mixture of three kinase inhibitors commonly used for kinase-enrichment increased the number of kinase identifications to 261, representing the largest kinome coverage from a single cell line reported to date. Coupling phosphopeptide enrichment with affinity purification using the four inhibitors enabled the identification of 799 high-confidence phosphosites on 183 kinases, ~10% of which were localized to the activation loop, and included previously unreported phosphosites on BMP2K, MELK, HIPK2, and PRKDC. Therefore, CTx-0294885 represents a powerful new reagent for analysis of kinome signaling networks that may facilitate development of targeted therapeutic strategies.

Name 2-((5-chloro-2-((4-(piperazin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)-N-methylbenzamide
Synonyms Benzamide, 2-[[5-chloro-2-[[4-(1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]-N-methyl-
CTx-0294885
CTX0294885
2-[(5-Chloro-2-{[4-(1-piperazinyl)phenyl]amino}-4-pyrimidinyl)amino]-N-methylbenzamide
Description CTX-0294885 is a a novel bisanilino pyrimidine; exhibits inhibitory activity against a broad range of kinases in vitro, and further developed it into a Sepharose-supported kinase capture reagent.Target: Kinase capture reagentUse of a quantitative proteomics approach confirmed the selectivity of CTx-0294885-bound beads for kinase enrichment. Large-scale CTx-0294885-based affinity purification followed by LC-MS/MS led to the identification of 235 protein kinases from MDA-MB-231 cells, including all members of the AKT family that had not been previously detected by other broad-spectrum kinase inhibitors. Addition of CTx-0294885 to a mixture of three kinase inhibitors commonly used for kinase-enrichment increased the number of kinase identifications to 261, representing the largest kinome coverage from a single cell line reported to date. Coupling phosphopeptide enrichment with affinity purification using the four inhibitors enabled the identification of 799 high-confidence phosphosites on 183 kinases, ~10% of which were localized to the activation loop, and included previously unreported phosphosites on BMP2K, MELK, HIPK2, and PRKDC. Therefore, CTx-0294885 represents a powerful new reagent for analysis of kinome signaling networks that may facilitate development of targeted therapeutic strategies.
Related Catalog
References

[1]. Zhang L, et al. Characterization of the novel broad-spectrum kinase inhibitor CTx-0294885 as an affinity reagent for mass spectrometry-based kinome profiling. J Proteome Res. 2013 Jul 5;12(7):3104-16.

Density 1.3±0.1 g/cm3
Molecular Formula C22H24ClN7O
Molecular Weight 437.925
Exact Mass 437.173096
PSA 94.21000
LogP 2.22
Appearance off white solid
Index of Refraction 1.674
Storage condition -20℃