Discovery of dabrafenib: A selective inhibitor of Raf Kinases with antitumor activity against B-Raf-driven tumors
Publication
, Journal Article
Rheault, TR; Stellwagen, JC; Adjabeng, GM; Hornberger, KR; Petrov, KG; Waterson, AG; Dickerson, SH; Mook, RA; Laquerre, SG; King, AJ; Han, C ...
Published in: ACS Medicinal Chemistry Letters
March 14, 2013
Hyperactive signaling of the MAP kinase pathway resulting from the constitutively active B-RafV600E mutated enzyme has been observed in a number of human tumors, including melanomas. Herein we report the discovery and biological evaluation of GSK2118436, a selective inhibitor of Raf kinases with potent in vitro activity in oncogenic B-Raf-driven melanoma and colorectal carcinoma cells and robust in vivo antitumor and pharmacodynamic activity in mouse models of B-RafV600E human melanoma. GSK2118436 was identified as a development candidate, and early clinical results have shown significant activity in patients with B-Raf mutant melanoma. © 2013 American Chemical Society.
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Published In
ACS Medicinal Chemistry Letters
DOI
EISSN
1948-5875
Publication Date
March 14, 2013
Volume
4
Issue
3
Start / End Page
358 / 362
Related Subject Headings
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
- 1115 Pharmacology and Pharmaceutical Sciences
- 0305 Organic Chemistry
- 0304 Medicinal and Biomolecular Chemistry
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Rheault, T. R., Stellwagen, J. C., Adjabeng, G. M., Hornberger, K. R., Petrov, K. G., Waterson, A. G., … Uehling, D. E. (2013). Discovery of dabrafenib: A selective inhibitor of Raf Kinases with antitumor activity against B-Raf-driven tumors. ACS Medicinal Chemistry Letters, 4(3), 358–362. https://doi.org/10.1021/ml4000063
Rheault, T. R., J. C. Stellwagen, G. M. Adjabeng, K. R. Hornberger, K. G. Petrov, A. G. Waterson, S. H. Dickerson, et al. “Discovery of dabrafenib: A selective inhibitor of Raf Kinases with antitumor activity against B-Raf-driven tumors.” ACS Medicinal Chemistry Letters 4, no. 3 (March 14, 2013): 358–62. https://doi.org/10.1021/ml4000063.
Rheault TR, Stellwagen JC, Adjabeng GM, Hornberger KR, Petrov KG, Waterson AG, et al. Discovery of dabrafenib: A selective inhibitor of Raf Kinases with antitumor activity against B-Raf-driven tumors. ACS Medicinal Chemistry Letters. 2013 Mar 14;4(3):358–62.
Rheault, T. R., et al. “Discovery of dabrafenib: A selective inhibitor of Raf Kinases with antitumor activity against B-Raf-driven tumors.” ACS Medicinal Chemistry Letters, vol. 4, no. 3, Mar. 2013, pp. 358–62. Scopus, doi:10.1021/ml4000063.
Rheault TR, Stellwagen JC, Adjabeng GM, Hornberger KR, Petrov KG, Waterson AG, Dickerson SH, Mook RA, Laquerre SG, King AJ, Rossanese OW, Arnone MR, Smitheman KN, Kane-Carson LS, Han C, Moorthy GS, Moss KG, Uehling DE. Discovery of dabrafenib: A selective inhibitor of Raf Kinases with antitumor activity against B-Raf-driven tumors. ACS Medicinal Chemistry Letters. 2013 Mar 14;4(3):358–362.
Published In
ACS Medicinal Chemistry Letters
DOI
EISSN
1948-5875
Publication Date
March 14, 2013
Volume
4
Issue
3
Start / End Page
358 / 362
Related Subject Headings
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
- 1115 Pharmacology and Pharmaceutical Sciences
- 0305 Organic Chemistry
- 0304 Medicinal and Biomolecular Chemistry