BMS-509744

CAS No. 439575-02-7

BMS-509744 ( PD 0332991 )

Catalog No. M21885 CAS No. 439575-02-7

BMS-509744 is a potent, selective and ATP competitive Itk inhibitor with an IC50 of 19 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    BMS-509744
  • Note
    Research use only, not for human use.
  • Brief Description
    BMS-509744 is a potent, selective and ATP competitive Itk inhibitor with an IC50 of 19 nM.
  • Description
    BMS-509744 reduces T-cell receptor-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells. BMS-488516 and BMS-509744 potently inhibit Itk in vitro with IC50 values of 96 and 19 nM, respectively. Both compounds exhibit competitive kinetics with respect to ATP, suggesting that they bind to the ATP binding site of the Itk kinase domain.
  • Synonyms
    PD 0332991
  • Pathway
    Angiogenesis
  • Target
    CDK
  • Recptor
    MAPK/DYRK1A
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    439575-02-7
  • Formula Weight
    447.53
  • Molecular Formula
    C24H29N7O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 5 mg/mL (11.17 mM; ultrasonic and adjust pH to 3 with HCl);H2O : 0.1 mg/mL (0.22 mM; Need ultrasonic)
  • SMILES
    O=C1C(C(C)=O)=C(C2=CN=C(N=C2N1C3CCCC3)NC4=CC=C(N5CCNCC5)C=N4)C
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38. 2. Katsumi Y, et al. Sensitivity of malignant rhabdoid tumor cell lines to PD 0332991 is inversely correlated with p16 expression. Biochem Biophys Res Commun, 2011, 413(1), 62-68. 3. Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475.
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