PLX-4720

	产品编号	CFN60059
	CAS编号	918505-84-7
	分子式 = 分子量	C₁₇H₁₄ClF₂N₃O₃S = 413.83
	产品纯度	>=98%
	物理属性	Powder
	化合物类型	Alkaloids
	植物来源
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产品名称	产品编号	CAS编号	包装	QQ客服
PLX-4720	CFN60059	918505-84-7	1mg	QQ客服：3257982914
PLX-4720	CFN60059	918505-84-7	5mg	QQ客服：3257982914
PLX-4720	CFN60059	918505-84-7	10mg	QQ客服：3257982914
PLX-4720	CFN60059	918505-84-7	20mg	QQ客服：3257982914

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Description:

PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.

Targets:

B-RafV600E

In vitro:

Cancer Res,2011 Apr 1;71(7):2750-60.

PTEN loss confers BRAF inhibitor resistance to melanoma cells through the suppression of BIM expression.[Pubmed: 21317224]

This study addresses the role of PTEN loss in intrinsic resistance to the BRAF inhibitor PLX4720.
METHODS AND RESULTS:
Immunohistochemical staining of a tissue array covering all stages of melanocytic neoplasia (n = 192) revealed PTEN expression to be lost in >10% of all melanoma cases. Although PTEN expression status did not predict for sensitivity to the growth inhibitory effects of PLX4720, it was predictive for apoptosis, with only limited cell death observed in melanomas lacking PTEN expression (PTEN-). Mechanistically, PLX4720 was found to stimulate AKT signaling in the PTEN- but not the PTEN+ cell lines. Liquid chromatography multiple reaction monitoring mass spectrometry (LC-MRM) was performed to identify differences in apoptosis signaling between the two cell line groups. PLX4720 treatment significantly increased BIM expression in the PTEN+ (>14-fold) compared with the PTEN- cell lines (four-fold). A role for PTEN in the regulation of PLX4720-mediated BIM expression was confirmed by siRNA knockdown of PTEN and through reintroduction of PTEN into cells that were PTEN-. Further studies showed that siRNA knockdown of BIM significantly blunted the apoptotic response in PTEN+ melanoma cells. Dual treatment of PTEN- cells with PLX4720 and a PI3K inhibitor enhanced BIM expression at both the mRNA and protein level and increased the level of apoptosis through a mechanism involving AKT3 and the activation of FOXO3a.
CONCLUSIONS:
In conclusion, we have shown for the first time that loss of PTEN contributes to intrinsic BRAF inhibitor resistance via the suppression of BIM-mediated apoptosis.

In vivo:

Proc Natl Acad Sci U S A,2010 Jun 8;107(23):10649-54.

B-Raf(V600E) and thrombospondin-1 promote thyroid cancer progression.[Pubmed: 20498063]

Although B-Raf(V600E) is the most common somatic mutation in papillary thyroid carcinoma (PTC), how it induces tumor aggressiveness is not fully understood.
METHODS AND RESULTS:
Using gene set enrichment analysis and in vitro and in vivo functional studies, we identified and validated a B-Raf(V600E) gene set signature associated with tumor progression in PTCs. An independent cohort of B-Raf(V600E)-positive PTCs showed significantly higher expression levels of many extracellular matrix genes compared with controls. We performed extensive in vitro and in vivo validations on thrombospondin-1 (TSP-1), because it has been previously shown to be important in the regulation of tumor angiogenesis and metastasis and is present in abundance in tumor stroma. Knockdown of B-Raf(V600E) resulted in TSP-1 down-regulation and a reduction of adhesion and migration/invasion of human thyroid cancer cells. Knockdown of TSP-1 resulted in a similar phenotype. B-Raf(V600E) cells in which either B-Raf(V600E) or TSP-1 were knocked down were implanted orthotopically into the thyroids of immunocompromised mice, resulting in significant reduction in tumor size and fewer pulmonary metastases from the primary carcinoma as compared with the control cells. Treatment of orthotopic thyroid tumors, initiated 1 week after tumor cell implantation with PLX4720, an orally available selective inhibitor of B-Raf(V600E), caused a significant tumor growth delay and decreased distant metastases, without evidence of toxicity.
CONCLUSIONS:
In conclusion, B-Raf(V600E) plays an important role in PTC progression through genes (i.e., TSP-1) important in tumor invasion and metastasis. Testing of a patient's thyroid cancer for B-Raf(V600E) will yield important information about potential tumor aggressiveness and also allow for future use of targeted therapies with selective B-Raf(V600E) inhibitors, such as PLX4720.

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	2.4165 mL	12.0823 mL	24.1645 mL	48.329 mL	60.4113 mL
5 mM	0.4833 mL	2.4165 mL	4.8329 mL	9.6658 mL	12.0823 mL
10 mM	0.2416 mL	1.2082 mL	2.4165 mL	4.8329 mL	6.0411 mL
50 mM	0.0483 mL	0.2416 mL	0.4833 mL	0.9666 mL	1.2082 mL
100 mM	0.0242 mL	0.1208 mL	0.2416 mL	0.4833 mL	0.6041 mL

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Corylifol A; Corylifol A	CFN92226	775351-88-7	C₂₅H₂₆O₄ = 390.5	20mg	QQ客服：2159513211
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Sarracenin; Sarracenin	CFN93043	59653-37-1	C₁₁H₁₄O₅ = 226.22	10mg	QQ客服：2159513211
异风藤奎醇A; Isofutoquinol A	CFN91836	62499-70-1	C₂₁H₂₂O₅ = 354.4	5mg	QQ客服：215959384

PLX-4720

PLX-4720

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