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Catalog #:

IN0012-5mg USD150.0
IN0012-25mg USD594.0

References for GDC-0449:

1. LoRusso, P. M., Rudin, C. M., Reddy, J. C., Tibes, R., Weiss, G. J., Borad, M. J., Hann, C. L., Brahmer, J. R., Chang, I., Darbonne, W. C., Graham, R. A., Zerivitz, K. L., Low, J. A., and Von Hoff, D. D. Phase I trial of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with refractory, locally advanced or metastatic solid tumors. Clin Cancer Res, 17: 2502-2511.

2. Graham, R. A., Lum, B. L., Cheeti, S., Jin, J. Y., Jorga, K., Von Hoff, D. D., Rudin, C. M., Reddy, J. C., Low, J. A., and Lorusso, P. M. Pharmacokinetics of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with locally advanced or metastatic solid tumors: the role of alpha-1-acid glycoprotein binding. Clin Cancer Res, 17: 2512-2520.

3. Dijkgraaf, G. J., Alicke, B., Weinmann, L., Januario, T., West, K., Modrusan, Z., Burdick, D., Goldsmith, R., Robarge, K., Sutherlin, D., Scales, S. J., Gould, S. E., Yauch, R. L., and de Sauvage, F. J. Small molecule inhibition of GDC-0449 refractory smoothened mutants and downstream mechanisms of drug resistance. Cancer Res, 71: 435-444.

4. Amin, S. H., Tibes, R., Kim, J. E., and Hybarger, C. P. Hedgehog antagonist GDC-0449 is effective in the treatment of advanced basal cell carcinoma. Laryngoscope, 120: 2456-2459.

5. Wong, H., Theil, F. P., Cui, Y., Marsters, J. C., Jr., Khojasteh, S. C., Vernillet, L., La, H., Song, X., Wang, H., Morinello, E. J., Deng, Y., and Hop, C. E. Interplay of dissolution, solubility, and nonsink permeation determines the oral absorption of the Hedgehog pathway inhibitor GDC-0449 in dogs: an investigation using preclinical studies and physiologically based pharmacokinetic modeling. Drug Metab Dispos, 38: 1029-1038.

6. Ding, X., Chou, B., Graham, R. A., Cheeti, S., Percey, S., Matassa, L. C., Reuschel, S. A., Meng, M., Liu, S., Voelker, T., Lum, B. L., Rudewicz, P. J., and Hop, C. E. Determination of GDC-0449, a small-molecule inhibitor of the Hedgehog signaling pathway, in human plasma by solid phase extraction-liquid chromatographic-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci, 878: 785-790.

7. Doggrell, S. A. The hedgehog pathway inhibitor GDC-0449 shows potential in skin and other cancers. Expert Opin Investig Drugs, 19: 451-454.

8. Dierks, C. GDC-0449--targeting the hedgehog signaling pathway. Recent Results Cancer Res, 184: 235-238.

9. Wong, H., Chen, J. Z., Chou, B., Halladay, J. S., Kenny, J. R., La, H., Marsters, J. C., Jr., Plise, E., Rudewicz, P. J., Robarge, K., Shin, Y., Wong, S., Zhang, C., and Khojasteh, S. C. Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide) , an orally bioavailable systemic Hedgehog signalling pathway inhibitor. Xenobiotica, 39: 850-861, 2009.

10. Rudin, C. M., Hann, C. L., Laterra, J., Yauch, R. L., Callahan, C. A., Fu, L., Holcomb, T., Stinson, J., Gould, S. E., Coleman, B., LoRusso, P. M., Von Hoff, D. D., de Sauvage, F. J., and Low, J. A. Treatment of medulloblastoma with hedgehog pathway inhibitor GDC-0449. N Engl J Med, 361: 1173-1178, 2009.

11. Robarge, K. D., Brunton, S. A., Castanedo, G. M., Cui, Y., Dina, M. S., Goldsmith, R., Gould, S. E., Guichert, O., Gunzner, J. L., Halladay, J., Jia, W., Khojasteh, C., Koehler, M. F., Kotkow, K., La, H., Lalonde, R. L., Lau, K., Lee, L., Marshall, D., Marsters, J. C., Jr., Murray, L. J., Qian, C., Rubin, L. L., Salphati, L., Stanley, M. S., Stibbard, J. H., Sutherlin, D. P., Ubhayaker, S., Wang, S., Wong, S., and Xie, M. GDC-0449-a potent inhibitor of the hedgehog pathway. Bioorg Med Chem Lett, 19: 5576-5581, 2009.

Certificate of Analysis/MSDS is available upon request with lot number

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