Compound 401 (CAS 168425-64-7)

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Ansökan Compound 401 is a selective inhibitor of DNA-PK and FRAP

CAS Nr: 168425-64-7

Renhet: >95%

Molekylvikt: 281.3

Molekylär formel: C₁₆H₁₅N₃O₂

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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Compound 401 is a cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC₅₀ = 280 nM) with ~19-fold selectivity over mTOR (FRAP) (IC₅₀ = 5.3 μM). Compound 401 exhibits much reduced or no activity against 43 other commonly studied kinases, including PI 3-K, ATM, and ATR. Compound 401 has been shown to induce apoptosis and inhibit FRAP-dependent growth in TSC1-/- murine embryo fibroblasts.

Konferenser

Ballou, L.M., et al. 2007. J. Biol. Chem. 282, 24463. Griffin, R.J., et al. 2005. J. Med. Chem. 48, 569

Physical State :

Solid

Solubility :

Soluble in DMSO (5 mg/ml), and ethanol (5 mM).

LAGRING :

Store at 4° C

Melting Point :

187.05° C (Predicted)

Boiling Point :

456.92° C at 760 mmHg (Predicted)

Density :

1.36 g/cm³ (Predicted)

Refractive Index :

n²⁰_D 1.70 (Predicted)

IC50 :

DNA-PK: IC₅₀ = 0.28 µM; mTOR: IC₅₀ = 5.3 µM; FK506 binding protein 12: IC₅₀ = 5.3 µM (human); PI 3-K: IC₅₀ = >100 µM; ATM: IC₅₀ = >100 µM; ATR: IC₅₀ = >100 µM

pK Values :

pK_b: 1.01

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

PubChem CID :

25817490

MDL Number :

MFCD10568147

SMILES :

C1COCCN1C2=CC(=O)[N+]3=C(N2)C4=CC=CC=C4C=C3

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Certificate of Analysis

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Compound 401 (CAS 168425-64-7) Produkt Citat

See how others have used Compound 401 (CAS 168425-64-7). Click on the entry to view the PubMed entry .

Citations 1 to 4 of 4 total

PMID: # 23373904 Shepelev, MV. et al. 2013. Mol. Pharm. 10: 931-9.

PMID: # 17562705 Ballou, LM. et al. 2007. J. Biol. Chem. 282: 24463-24470.

PMID: # 12941142 Tamai, R. et al. 2003. Immunology. 110: 66-72.

PMID: # 1937825 Wang, MH. et al. 1991. Infect. Immun. 59: 4655-4664.

Citations 1 to 4 of 4 total

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