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PP2 (kinase inhibitor)

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PP2 (kinase inhibitor)
Names
IUPAC name (4-amino-5-(4-chlorophenyl)-7-(dimethylethyl)pyrazolopyrimidine
Identifiers
CAS Number
3D model (JSmol)
PubChem CID
CompTox Dashboard (EPA)
InChI
  • InChI=1S/C15H16ClN5/c1-15(2,3)21-14-11(13(17)18-8-19-14)12(20-21)9-4-6-10(16)7-5-9/h4-8H,1-3H3,(H2,17,18,19)
SMILES
  • Nc2ncnc(c12)n(C(C)(C)C)nc1-c3ccc(Cl)cc3
Properties
Chemical formula C15H16ClN5
Molar mass 301.774
Appearance white to off-white solid
Solubility in DMSO 25 mg/ml
Except where otherwise noted, data are given for materials in their standard state (at 25 °C , 100 kPa). checkY verify (what is  ?) Infobox references
Chemical compound

PP2 is a substance used in cancer research as a selective inhibitor for Src-family kinases. It strongly inhibits the kinases Lck (IC50=4 nM), Fyn (5 nM) and Hck (5 nM), shows weaker inhibition of EGFR (480 nM) and practically no inhibition of ZAP-70 (100 µM) and JAK2 (50 µM).

References

  1. Hanke, JH; Gardner, JP; Dow, RL; Changelian, PS; Brissette, WH; Weringer, EJ; Pollok, BA; Connelly, PA (1996). "Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation". The Journal of biological chemistry. 271 (2): 695–701. PMID 8557675.
  2. Chen, JK; Capdevila, J; Harris, RC (2000). "Overexpression of C-terminal Src kinase blocks 14, 15-epoxyeicosatrienoic acid-induced tyrosine phosphorylation and mitogenesis". The Journal of biological chemistry. 275 (18): 13789–92. doi:10.1074/jbc.275.18.13789. PMID 10788500.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  3. Yoshizumi, M; Abe, J; Haendeler, J; Huang, Q; Berk, BC (2000). "Src and Cas mediate JNK activation but not ERK1/2 and p38 kinases by reactive oxygen species". The Journal of biological chemistry. 275 (16): 11706–12. doi:10.1074/jbc.275.16.11706. PMID 10766791.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  4. Carlomagno, F; Vitagliano, D; Guida, T; Basolo, F; Castellone, MD; Melillo, RM; Fusco, A; Santoro, M (2003). "Efficient inhibition of RET/papillary thyroid carcinoma oncogenic kinases by 4-amino-5-(4-chloro-phenyl)-7-(t-butyl)pyrazolo3,4-dpyrimidine (PP2)". The Journal of clinical endocrinology and metabolism. 88 (4): 1897–902. doi:10.1210/jc.2002-021278. PMID 12679489.
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