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About This Item
Empirical Formula (Hill Notation):
C16H19N5
CAS Number:
Molecular Weight:
281.36
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.77
Quality Level
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
off-white
solubility
DMSO: 25 mg/mL
storage temp.
−20°C
SMILES string
[n]1(nc(c3c1ncnc3N)c2ccc(cc2)C)C(C)(C)C
InChI
1S/C16H19N5/c1-10-5-7-11(8-6-10)13-12-14(17)18-9-19-15(12)21(20-13)16(2,3)4/h5-9H,1-4H3,(H2,17,18,19)
InChI key
ZVPDNRVYHLRXLX-UHFFFAOYSA-N
General description
A cell-permeable pyrazolopyrimidine compound that is shown to inhibit Src family tyrosine kinases Lck, Fyn, Hck, and Src (IC50 = 5, 6, 20, and 170 nM, respectively), as well as non-Src family kinases such as CSK, RIP2, and CK1δ (IC50 = 640 nM, 26 nM, 170 nM, respectively), in in vitro kinase assays. At 1 µM, in vitro kinase activity is reduced by more than 57% for p38α, p38β, CK1δ, CSK, RIP2, and GAK, while exhibiting much lower activity against more than 60 other kinases. Kinetic studies employing Src and [poly Glu-Tyr 4:1] indicate that the inhibition is mixed competitive with respect to the substrate and non-competitive with respect to ATP. PP1 also demonstrates anti-growth properties in several B lymphoma cultures of human and murine origins (IC50 = 2.5 to 8.0 µM) and pediatric brain tumor cells (IC50 = 1.1 to 9.7 µM). Also available in InSolution format (Cat. No. 539741).
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Ke, J., et.al. 2009. Mol. Cancer8, 132.
Sikkema, A.H., et al. 2009. Cancer Res.69, 5987.
Bain, J., et al. 2007. Biochem. J.408, 297.
Bain, J., et al. 2003. Biochem. J.371, 199.
Karni, R., et al. 2003. FEBS Lett.537, 47.
Hanke, J.H., et al. 1996. J. Biol. Chem.271, 695.
Sikkema, A.H., et al. 2009. Cancer Res.69, 5987.
Bain, J., et al. 2007. Biochem. J.408, 297.
Bain, J., et al. 2003. Biochem. J.371, 199.
Karni, R., et al. 2003. FEBS Lett.537, 47.
Hanke, J.H., et al. 1996. J. Biol. Chem.271, 695.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
Certificates of Analysis (COA)
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Global Trade Item Number
| SKU | GTIN |
|---|---|
| 567809-1MG | 04055977190373 |
