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 |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Apsel et al (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat.Chem.Biol. 4 691 PMID: 18849971
Keywords: PP 121, supplier, PP121, PI, 3-K, PI, 3-kinase, PI3K, dual, inhibitors, inhibits, receptor, tyrosine, kinases, RTKs, PI, 3-Kinase, mTOR, Other, RTKs, PI, 3-Kinase, Tocris Bioscience
