PI-103 (CAS 371935-74-9)

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Alternativa namn: PI 3-K Inhibitor V

Ansökan PI-103 is an ATP-competitive DNA-PK, PI 3-kinase, and FRAP inhibitor

CAS Nr: 371935-74-9

Renhet: 99%

Molekylvikt: 348.36

Molekylär formel: C₁₉H₁₆N₄O₃

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

* 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.

Konferenser

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.

LAGRING :

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 :

n²⁰_D 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: K_i= 2 µM; p33cdk2/cyclin E: K_i= 2 µM

pK Values :

pK_a: 9.06 (Predicted), pK_b: 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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Certificate of Analysis

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PI-103 (CAS 371935-74-9) Produkt Citat

See how others have used PI-103 (CAS 371935-74-9). Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

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

PMID: # 26355082 Kwon, YC. et al. 2015. J. Virol. 89: 11549-56.

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

Citations 1 to 3 of 3 total

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