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Chemical Structure| 90213-66-4 Chemical Structure| 90213-66-4
Chemical Structure| 90213-66-4

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Synonyms: 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine

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Product Citations

Joel Rüegger ; Berend Gagestein ; Antonius P. A. Janssen ; Alexandra Valeanu ; Alger Lazo Mori ; Marielle van der Peet , et al.

Abstract: The human genome encodes 518 protein kinases that are pivotal for drug discovery in various therapeutic areas such as cancer and autoimmune disorders. The majority of kinase inhibitors target the conserved ATP-binding pocket, making it difficult to develop selective inhibitors. To characterize and prioritize kinase-inhibiting drug candidates, efficient methods are desired to determine target engagement across the cellular kinome. In this study, we present CellEKT (Cellular Endogenous Kinase Targeting), an optimized and robust chemical proteomics platform for investigating cellular target engagement of endogenously expressed kinases using the sulfonyl fluoride-based probe XO44 and two new probes ALX005 and ALX011. The optimized workflow enabled the determination of the kinome interaction landscape of covalent and non-covalent drugs across over 300 kinases, expressed as half maximum inhibitory concentration (IC50), which were validated using distinct platforms like phosphoproteomics and NanoBRET. With CellEKT, target engagement profiles were linked to their substrate space. CellEKT has the ability to decrypt drug actions and to guide the discovery and development of drugs.

Keywords: CellEKT ; cellular target engagement ; endogenous kinome profiling ; XO44 ; IC50 ; drug selectivity ; broadspectrum kinase probes ; chemical proteomics ; ABPP

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Product Details of 2,6-Dichloro-7-deazapurine

CAS No. :90213-66-4
Formula : C6H3Cl2N3
M.W : 188.01
SMILES Code : ClC1=C2C(NC=C2)=NC(Cl)=N1
Synonyms :
2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine
MDL No. :MFCD08059278
InChI Key :GHXBPCSSQOKKGB-UHFFFAOYSA-N
Pubchem ID :14116871

Safety of 2,6-Dichloro-7-deazapurine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P261-P280-P305+P351+P338

Application In Synthesis of 2,6-Dichloro-7-deazapurine

* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.

  • Upstream synthesis route of [ 90213-66-4 ]
  • Downstream synthetic route of [ 90213-66-4 ]

[ 90213-66-4 ] Synthesis Path-Upstream   1~1

  • 1
  • [ 90213-66-4 ]
  • [ 1192711-88-8 ]
References: [1] Patent: WO2009/131687, 2009, A2, . Location in patent: Page/Page column 148.
 

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