Dabrafenib

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本试剂(Dabrafenib)
仅供科研实验使用,不得用于其他用途！

简介：
货 号：D-5678
名 称：Dabrafenib
别 名：Dabrafenib Free Base
C A S ：1195765-45-7
分子量：519.56
分子式：C23H20F3N5O2S2
纯 度：HPLC/TLC:>99%
说 明：
文 献：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).