Description: Dual kinase inhibitor; inhibits PI 3-K family kinases
Chemical Name: 1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μM for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μM for p110α, DNA-PK and mTOR). Exhibits no significant effect on receptor serine/threonine kinases (RSTKs). Blocks the proliferation of tumor cells by direct inhibition of PI 3-K, mTOR, Src and the VEGF receptor.
Compound Libraries
PP 121 is also offered as part of the
Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
M. Wt
319.36
Formula
C17H17N7
Storage
Store at +4°C
Purity
≥99% (HPLC)
CAS Number
1092788-83-4
PubChem ID
24905142
InChI Key
NVRXTLZYXZNATH-UHFFFAOYSA-N
Smiles
NC1=C2C(N(C5CCCC5)N=C2C3=CN=C(NC=C4)C4=C3)=NC=N1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
31.94
100
ethanol
15.97
50
Preparing Stock Solutions
The following data is based on the product molecular weight 319.36. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
3.13 mL
15.66 mL
31.31 mL
5 mM
0.63 mL
3.13 mL
6.26 mL
10 mM
0.31 mL
1.57 mL
3.13 mL
50 mM
0.06 mL
0.31 mL
0.63 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Apselet al (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat.Chem.Biol. 4 691 PMID: 18849971