PI-103An ATP-competitive DNA-PK, PI 3-kinase, and FRAP inhibitor

PI-103 (CAS 371935-74-9)

PI-103 | CAS 371935-74-9 is rated 5.0 out of 5 by 1.
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Synonym: PI 3-K Inhibitor V
Application: An ATP-competitive DNA-PK, PI 3-kinase, and FRAP inhibitor
CAS Number: 371935-74-9
Purity: 99%
Molecular Weight: 348.36
Molecular Formula: C19H16N4O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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PI-103 is a cell-permeable pyridinylfuranopyrimidine compound that acts as an ATP-competitive inhibitor of DNA-PK, PI 3-kinase (Class IA), and FRAP (mTOR) complex 1 and 2. Studies suggest that PI-103 can induce apoptosis and an arrest in the cell cycle by inhibition of the aforementioned proteins. When PI-103 is combined with rapamycin, a prototypic mTORC1 inhibitor, synergistic suppression of AKT and ribosomal S6 protein phosphorylation are observed. In addition, PI-103 has been seen to have nominal effects inhibiting basal Na+ transport, but is very effective in abolishing insulin-induced Na+ absorption in the nephron.


References

1. Demyanets, S., et al. 2010. Basic Res Cardiol. [Epub ahead of print]. PMID: 21174212
2. Mansley, M.K., et al. 2010. Br. J. Pharmacol. 161: 571-588. PMID: 20880397
3. Bagci-Onder, T., et al. 2010. Cancer Res. [Epub ahead of print]. PMID: 21084267
4. Werzowa, J., et al. 2010. J. Invest. Dermatol. [Epub ahead of print]. PMID: 21048785

Physical State :
Solid
Solubility :
Soluble in DMSO (10 mg/ml), DMF (10 mg/ml), 1:2 DMSO:PBS(pH 7.2) (0.25 mg/ml), water (<1 mg/ml) at 25° C, and ethanol (<1 mg/ml) at 25° C.
Storage :
Store at -20° C
Melting Point :
231.64° C (Predicted)
Boiling Point :
520.25° C at 760 mmHg (Predicted)
Density :
1.41 g/cm3 (Predicted)
Refractive Index :
n20D 1.71
IC50 :
DNA-PK: IC50 = 2 nM; p110α: IC50 = 8 nM; p110β: IC50 = 88 nM; p110δ: IC50 = 48 nM; p110γ: IC50 = 150 nM; PI3-KC2β: IC50 = 26 nM; mTORC1: IC50 = 20 nM; mTORC2: IC50 = 83 nM; ATR: IC50 = 850 nM; ATM: IC50 = 920 nM; PI 3-KC2α: IC50 = ~ 1 µM; hsVPS34: IC50 = 2.3 µM
Ki Data :
Cdk5/p25: Ki= 2 µM; p33cdk2/cyclin E: Ki= 2 µM
pK Values :
pKa: 9.06 (Predicted), pKb: 2.97 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
9884685
MDL Number :
MFCD11983145
SMILES :
C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O

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PI-103  Product Citations

See how others have used PI-103. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 30731136  Höllerhage, M. et al. 2019. Neuropharmacology. 149: 13-26.

PMID: # 17804702  Fan, QW. et al. 2007. Cancer Res. 67(17): 7960-7965.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Fan Fan, QW. et al. (PubMed 17804702) used PI-103, an ATP-competitive dual inhibitor of Class IA PI3K and mTOR complex 1 and 2, to increase the efficacy of erlotinib against EGFR-driven glioma cell lines containing mutant PTEN. Introduction of PI-103 significantly increased erlotinib anti-proliferative efficacy in mutant PTEN glioma cell lines. -SCBT Publication Review
Date published: 2015-02-23
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