英国Kinasechem现货PLX-4720 CAS No. 918505-84-7

货号：	K1053
保质期：	2年
保存条件：	-20℃
供应商：	Kinasechem
CAS号：	918505-84-7
英文名：	PLX-4720
规格：	5G/2mg/5mg/10mg

MW：413.83
溶解性：DSMO 83 mg/mL Water <1 mg/ml Ethanol <1 mg/ml
纯度：>99%
描述：
PLX-4720 is a B-raf and c-raf inhibitor with IC50 of 13 nM and 6.7 nM. Activating mutations in B-RAF and N-RAS occur in approximately 60 and approximately 15% of melanomas, respectively. The most common mutation in B-RAF is V600E, which activates B-RAF and the downstream MEK-ERK1/2 pathway. Thus, B-RAF(V600E) is a viable therapeutic target. PLX4720 is a selective inhibitor of mutant B-RAF and its analog, PLX4032, is currently undergoing clinical trials in melanoma. The effects of PLX4720 across the genotypic spectrum in melanoma remain unclear. PLX4720 treatment rapidly induces hyperactivation of the MEK-ERK1/2 pathway in mutant N-RAS melanoma cells. And PLX4720-induced hyperactivation of the MEK-ERK1/2 pathway promotes resistance to apoptosis in both non-invasive and invasive mutant N-RAS melanoma cells but does not enhance cell cycle properties. Combination of thyroidectomy and PLX4720 can extend survival and would decrease tumor burden in a mouse model. As B-Raf(V600E) is a frequent mutation in anaplastic thyroid cancers and is a novel therapeutic target, it could be an effective therapeutic strategy for early anaplastic thyroid cancers that harbor the B-Raf(V600E) mutation and are refractory to conventional therapeutic modalities.
参考文献：
[1] Nehs, M. A., S. Nagarkatti, et al. (2010). "Thyroidectomy with neoadjuvant PLX4720 extends survival and decreases tumor burden in an orthotopic mouse model of anaplastic thyroid cancer." Surgery 148(6): 1154-1162; discussion 1162.
[2]Jiang, C. C., F. Lai, et al. (2011). "MEK-independent survival of B-RAFV600E melanoma cells selected for resistance to apoptosis induced by the RAF inhibitor PLX4720." Clin Cancer Res 17(4): 721-730.
[3] Kaplan, F. M., Y. Shao, et al. (2011). "Hyperactivation of MEK-ERK1/2 signaling and resistance to apoptosis induced by the oncogenic B-RAF inhibitor, PLX4720, in mutant N-RAS melanoma cells." Oncogene 30(3): 366-371.
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