Oxindole IA potent, selective inhibitor of VEGF

Oxindole I

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Synonym: 3-(1H-Pyrrol-2-ylmethylene)-1,3-dihydroindol-2-one
Application: A potent, selective inhibitor of VEGF
Molecular Weight: 210.2
Molecular Formula: C13H10N2O
* Refer to Certificate of Analysis for lot specific data (including water content).
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Oxindole I is a potent and selective inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinase Flk-1 (fetal liver kinase-1; IC50 = 390 nM). Also, to a lesser extent, it inhibits PDGFR (platelet derived growth factor receptor) kinase (IC50 = 12 μM). However, Oxindole I does not affect EGFR, HER2, and IGF-1R even at high concentrations (>100 μM). Oxindole I also inhibits cyclin D1/Cdk4 enzyme (IC50 = 4.9 μM) preferentially over cyclin E/Cdk2 (IC50 = 10 μM) and cyclin B/Cdk1 (IC50 = 10.2 μM).


References

1. Kent, L L., et al., 1999. Characterization of novel inhibitors of cyclin-dependent kinases. Biochemical and biophysical research communications. 260(3): 768-74. PMID: 10403840
2. Vieth, M., et al., 2000. DoMCoSAR: a novel approach for establishing the docking mode that is consistent with the structure-activity relationship. Application to HIV-1 protease inhibitors and VEGF receptor tyrosine kinase inhibitors. Journal of medicinal chemistry. 43(16): 3020-32. PMID: 10956210

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mg/ml).
Storage :
Store at -20° C
Melting Point :
179.17° C (Predicted)
Boiling Point :
490.69° C at 760 mmHg (Predicted)
Density :
1.34 g/cm3 (Predicted)
Refractive Index :
n20D 1.73 (Predicted)
IC50 :
ZR-75-1: IC50 = 100 nM; Vascular endothelial growth factor receptor 2: IC50 = 140 nM (human); Flk-1 : IC50 = 390 nM; MCF-7: IC50 = 420 nM; Vascular endothelial growth factor receptor 1: IC50 = 0.39 µM (mouse); cyclin E/Cdk2: IC50 = 10 µM; cyclin B/Cdk1: IC50 = 10.2 µM; PDGFR kinase: IC50 = 12 µM; cyclin D1/Cdk4 enzyme: IC50 = 4.9 µM
pK Values :
pKa: 12.65 (Predicted), pKb: 0.17 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
5908088
MDL Number :
MFCD00118215
SMILES :
C1=CC=C2C(=C1)/C(=C/C3=CC=CN3)/C(=O)N2

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Certificate of Analysis

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Oxindole I  Product Citations

See how others have used Oxindole I. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 26188358  Zhou, W. et al. 2015. Oncotarget. 6: 21557-71.

PMID: # 25186293  Soggia, A. et al. 2014. Diabetologia. 57: 2348-56.

Citations 1 to 2 of 2 total
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