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Description: Potent PI3K inhibitor, also used in hPSCs mesendoderm differentiation
Chemical Name: N-(2,3-Dihydro-7,8-dimethoxyimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide
Purity: ≥98% (HPLC)
Biological Activity for PIK 90
PIK 90 is a potent inhibitor of PI 3-K α/γ/δ kinases (IC50 = 11, 18, 47, 58 and 64 nM against p110α, p110γ, PI 3-KC2α, p110δ and PI 3-KC2α, respectively) as well as PIKKs (IC50 = 13 nM against DNA-PK). It inhibits the fMLP-stimulated phosphorylation of Akt and impairs polarity and chemotaxis in dHL60 cells. It suppresses insulin-stimulated phosphorylation of Akt and rpS6 in 3T3-L1 adipocytes and L6 myotubes in vitro and prevents insulin-induced blood glucose reduction in mice in vivo. PIK 90 can be used in combination with other small molecules and proteins for mesendoderm induction in protocols to differentiate iPSCs into organ-specific mesenchyme.
Technical Data for PIK 90
| M. Wt | 351.36 |
| Formula | C18H17N5O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 677338-12-4 |
| PubChem ID | 135398491 |
| InChI Key | ZJAVHOMVDCMAMF-UHFFFAOYSA-N |
| Smiles | O=C(NC1=NC=2C(OC)=C(OC)C=CC2C3=NCCN13)C=4C=NC=CC4 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PIK 90
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 3.51 | 10 with gentle warming |
Preparing Stock Solutions for PIK 90
The following data is based on the product molecular weight 351.36. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 28.46 mL | 142.3 mL | 284.61 mL |
| 0.5 mM | 5.69 mL | 28.46 mL | 56.92 mL |
| 1 mM | 2.85 mL | 14.23 mL | 28.46 mL |
| 5 mM | 0.57 mL | 2.85 mL | 5.69 mL |
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Product Datasheets for PIK 90
References for PIK 90
References are publications that support the biological activity of the product.
Fan et al (2006) A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer cell 9 341 PMID: 16697955
Knight et al (2006) A pharmacological map of the PI3-K family defines a role for p110a in insulin signaling. Cell 125 733 PMID: 16647110
Kishimoto et al (2022) Directed differentiation of human pluripotent stem cells into diverse organ-specific mesenchyme of the digestive and respiratory systems. Nat.Protoc. 17 2699 PMID: 35978039
Keymeulen et al (2006) To stabilize neutrophil polarity, PIP3 and Cdc42 augment RhoA activity at the back as well as signals at the front. J.Cell Biol. 174 437 PMID: 16864657
If you know of a relevant reference for PIK 90, please let us know.
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