D-5678 Dabrafenib, Free Base, >99%

Synonyms : [GSK-2118436] [GSK-2118436A]

Related Terms : [Tafinlar]

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  • 10 mg
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  • 41
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  • 25 mg
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  • 64
  • 54
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  • 50 mg
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  • 71
  • 60
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  • 100 mg
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  • 119
  • 101
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  • 200 mg
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  • 185
  • 157
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  • 500 mg
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  • 272
  • 230
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  • 1 g
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  • 413
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  • 2 g
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  • 5 g
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  • 10 g
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  • M.W. 519.56
  • C23H20F3N5O2S2
  • [1195765-45-7]

Solubility: Soluble in DMSO.

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  • Dabrafenib, also known as GSK2118436, is a potent and selective BRAF inhibitor. It inhibited human wtBRAF, BRAF(V600E) and BRAF(V600K) kinase activities with IC50 values of 3.2, 0.6, and 0.5 nM, respectively, decreased MEK and ERK phosphorylation, and blocked cell proliferation. In a BRAF(V600E)-containing xenograft model of human melanoma, dabrafenib inhibited ERK activation and tumor growth. However, dabrafenib caused MAPK pathway activation in wild-type BRAF cells through CRAF (RAF1) signalling. King A.J., et al. "Dabrafenib; Preclinical Characterization, Increased Efficacy when Combined with Trametinib, while BRAF/MEK Tool Combination Reduced Skin Lesions." PLoS One 8: e67583 (2013).
  • This research compound is the free base form of dabrafenib. We also offer the methanesulfonate salt form of dabrafenib:  Cat. No. D-5699 Dabrafenib, Methanesulfonate Salt.
  • This dabrafenib product is the free base, whose CAS number is given above. The CAS number of the methanesulfonate salt form is 1195768-06-9.
  • Dabrafenib inhibited B-RafV600E kinase with an IC50 of 0.7 nM, inhibited pERK in SKMEL28 cells with an IC50 of 4 nM, and blocked SKMEL28 cell proliferation with an IC50 of 3 nM. It also dramatically inhibited tumor growth in mice bearing B-RafV600E human melanoma tumors. Rheault T.R. et al. "Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors." ACS Med. Chem. Lett., 4: 358–362 (2013).
  • Dabrafenib inhibited cell proliferation and MAPK pathway in melanoma cell lines carrying BRAFV600D and BRAFV600R mutations but had no significant anti-proliferative effect in a melanoma cell line carrying wild type BRAF. Gentilcore G., et al. "Effect of dabrafenib on melanoma cell lines harbouring the BRAF(V600D/R) mutations." BMC Cancer 13: 17 (2013).
  • The acquired resistance to the BRAF inhibitor dabrafenib in the A375 BRAFV600E and the YUSIT1 BRAFV600K melanoma cell lines was overcome by combinations of BRAF, MEK, and PI3K/mTOR inhibitors. Greger J.G., et al. "Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations." Mol. Cancer Ther. 11: 909-920 (2012).
  • A phase I clinical study showed that dabrafenib was tolerable, had activity against BRAFV600E and BRAFV600K melanoma, and had activity against melanoma metastases in the brain. Falchook G.S., et al. "Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial." Lancet 379: 1893-1901 (2012).
  • A phase 2 clinical trial demonstrated that dabrafenib had activity and an acceptable safety profile in patients with BRAFV600E melanoma and brain metastases. Long G.V., et al. "Dabrafenib in patients with Val600Glu or Val600Lys BRAF-mutant melanoma metastatic to the brain (BREAK-MB): a multicentre, open-label, phase 2 trial." Lancet Oncol. 13: 1087-1095 (2012).
  • A phase 3 trial in patients with BRAF(V600E)-mutated metastatic melanoma demonstrated dabrafenib significantly improved progression-free survival compared with dacarbazine. Hauschild A., et al. "Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial." Lancet 380: 358-365 (2012).
  • Dabrafenib (as the methanesulfonate salt) is the active ingredient in the drug product sold under the trade name Tafinlar®.  This drug has been approved in at least one country for use in patients with mutated metastatic melanoma. NOTE: THE DABRAFENIB SOLD BY LC LABORATORIES FOR RESEARCH IS NOT TAFINLAR®, AND IS NOT FOR HUMAN USE.

  • Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
  • Related CAS numbers: 1195768-06-9 for the mesylate salt.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.