维罗非尼

Vemurafenib (PLX4032)

	产品编号	CFN60058
	CAS编号	918504-65-1
	分子式 = 分子量	C₂₃H₁₈ClF₂N₃O₃S = 489.92
	产品纯度	>=98%
	物理属性	Powder
	化合物类型	Alkaloids
	植物来源
ChemFaces的产品在影响因子大于5的优秀和顶级科学期刊中被引用

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产品名称	产品编号	CAS编号	包装	QQ客服
维罗非尼	CFN60058	918504-65-1	1mg	QQ客服：3004468520
维罗非尼	CFN60058	918504-65-1	5mg	QQ客服：3004468520
维罗非尼	CFN60058	918504-65-1	10mg	QQ客服：3004468520
维罗非尼	CFN60058	918504-65-1	20mg	QQ客服：3004468520

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ChemFaces的产品在许多优秀和顶级科学期刊中被引用

Cell. 2018 Jan 11;172(1-2):249-261.e12.
doi: 10.1016/j.cell.2017.12.019.
IF=36.216(2019)

PMID: 29328914

Cell Metab. 2020 Mar 3;31(3):534-548.e5.
doi: 10.1016/j.cmet.2020.01.002.
IF=22.415(2019)

PMID: 32004475

Mol Cell. 2017 Nov 16;68(4):673-685.e6.
doi: 10.1016/j.molcel.2017.10.022.
IF=14.548(2019)

PMID: 29149595

ACS Nano. 2018 Apr 24;12(4): 3385-3396.
doi: 10.1021/acsnano.7b08969.
IF=13.903(2019)

PMID: 29553709

Nature Plants. 2016 Dec 22;3: 16206.
doi: 10.1038/nplants.2016.205.
IF=13.297(2019)

PMID: 28005066

Sci Adv. 2018 Oct 24;4(10): eaat6994.
doi: 10.1126/sciadv.aat6994.
IF=12.804(2019)

PMID: 30417089

Donald Danforth Plant Science Center (USA)

The Vancouver Prostate Centre (VPC) (Canada)

University of Mysore (India)

University of Liège (Belgium)

University of Fribourg (Switzerland)

Shanghai Institute of Organic Chemistry (China)

Medical University of South Carolina (USA)

University of Lodz (Poland)

Subang Jaya Medical Centre (Malaysia)

University of Leipzig (Germany)

St. Jude Children Research Hospital (USA)

Yale University (USA)

Seoul National University (Korea)

University of Hull (United Kingdom)

More...

Description:

Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.

Targets:

B-RafV600E | Autophagy

In vitro:

Nature,2012 Jan 26;483(7387):100-3.

Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR.[Pubmed: 22281684]

Inhibition of the BRAF(V600E) oncoprotein by the small-molecule drug PLX4032 (vemurafenib) is highly effective in the treatment of melanoma. However, colon cancer patients harbouring the same BRAF(V600E) oncogenic lesion have poor prognosis and show only a very limited response to this drug.
METHODS AND RESULTS:
To investigate the cause of the limited therapeutic effect of PLX4032 in BRAF(V600E) mutant colon tumours, here we performed an RNA-interference-based genetic screen in human cells to search for kinases whose knockdown synergizes with BRAF(V600E) inhibition. We report that blockade of the epidermal growth factor receptor (EGFR) shows strong synergy with BRAF(V600E) inhibition. We find in multiple BRAF(V600E) mutant colon cancers that inhibition of EGFR by the antibody drug cetuximab or the small-molecule drugs gefitinib or erlotinib is strongly synergistic with BRAF(V600E) inhibition, both in vitro and in vivo. Mechanistically, we find that BRAF(V600E) inhibition causes a rapid feedback activation of EGFR, which supports continued proliferation in the presence of BRAF(V600E) inhibition. Melanoma cells express low levels of EGFR and are therefore not subject to this feedback activation. Consistent with this, we find that ectopic expression of EGFR in melanoma cells is sufficient to cause resistance to PLX4032.
CONCLUSIONS:
Our data suggest that BRAF(V600E) mutant colon cancers (approximately 8-10% of all colon cancers), for which there are currently no targeted treatment options available, might benefit from combination therapy consisting of BRAF and EGFR inhibitors.

产品名称	产品编号	CAS编号	分子式 = 分子量	位单	联系QQ
槲皮素3-O-(6''-没食子酰基)-β-D-半乳糖苷; Quercetin 3-O-(6''-galloyl)-beta-D-galactopyranoside	CFN91065	53171-28-1	C₂₈H₂₄O₁₆ = 616.5	10mg	QQ客服：3004468087
坦度替尼; Tandutinib (MLN518)	CFN60446	387867-13-2	C₃₁H₄₂N₆O₄ = 562.7	5mg	QQ客服：3004468520
6',7'-二羟薄荷素; 6',7'-Dihydroxybergamottin	CFN98307	264234-05-1	C₂₁H₂₄O₆ = 372.4	10mg	QQ客服：3004468088
绵枣儿素; Scillascillin	CFN98869	52706-07-7	C₁₇H₁₂O₆ = 312.3	5mg	QQ客服：3004468091

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	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	2.0411 mL	10.2057 mL	20.4115 mL	40.823 mL	51.0287 mL
5 mM	0.4082 mL	2.0411 mL	4.0823 mL	8.1646 mL	10.2057 mL
10 mM	0.2041 mL	1.0206 mL	2.0411 mL	4.0823 mL	5.1029 mL
50 mM	0.0408 mL	0.2041 mL	0.4082 mL	0.8165 mL	1.0206 mL
100 mM	0.0204 mL	0.1021 mL	0.2041 mL	0.4082 mL	0.5103 mL