GDC-0449, SMO antagonist

$ 94.00

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  • G449-005, 5 mg94.00
  • G449-025, 25 mg294.00
  • G449-100, 100 mg994.00
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Source M.W.421.3 CAS No.879085-55-9
Structural InfoC19H14Cl2N2O3S
GDC-0449, SMO antagonist
ReconstitutionBefore reconstitution, we recommend a brief spin to drive down any material dislodged from the bottom of the tube.  The compound is soluble in DMSO.
StabilityThe powder is stable for at least 2 year if stored at -20 °C. The dissolved compound is stable for at least 1 month at 4 °C, but should be stored in aliquots at -20 °C for longer term. Protect from light.
PurityGreater than 99% as determined by LC/MS analysis. LC/MS and/or NMR data available upon request.
Biological ActivityIn a cell-based assay measuring the activation of the Gli-1 reporter gene, this compound gives IC50 of 5-20 nM.
Country of OriginUSA

GDC-0449 (Vismodegib) is potent antagonist of SMO (smoothened). This small molecule compound is a hedgehog pathway inhibitor by directly binding to SMO. This molecule has been developed by Genentech for clinical application against hedgehog-dependent cancers.

Ref: Robarge KD, et al. Bioorg Med Chem Lett. Oct 1 2009 19: 5576-81;  
van Hoff DD, et al. N Engl J Med. Sep 17, 2009 361: 1164-72;
Rudin CM et al. N Engl J Med. 2009 Sep 17; 361(12):1173-8.

Okabe S, Tauchi T, Tanaka Y, et al., Effects of the hedgehog inhibitor GDC-0449, alone or in combination with dasatinib, on
BCR-ABL-positive leukemia cells. Stem Cells Dev. 2012 Nov 1;21(16):2939-48.