维罗非尼
Vemurafenib (PLX4032)
| 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：2056216494 |
| 维罗非尼 |
CFN60058 |
918504-65-1 |
5mg |
QQ客服：2056216494 |
| 维罗非尼 |
CFN60058 |
918504-65-1 |
10mg |
QQ客服：2056216494 |
| 维罗非尼 |
CFN60058 |
918504-65-1 |
20mg |
QQ客服：2056216494 |
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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
我们的产品现已经出口到下面的研究机构与大学，并且还在增涨
The University of Newcastle (Australia)
University of Indonesia (Indonesia)
Centralised Purchases Unit (CPU), B.I.T.S (India)
Chulalongkorn University (Thailand)
Sri Sai Aditya Institute of Pharmaceutical Sciences and Research (India)
Institute of Tropical Disease Universitas Airlangga (Indonesia)
Biotech R&D Institute (USA)
Universidade de Franca (Brazil)
Heinrich-Heine-University Düsseldorf (Germany)
Michigan State University (USA)
University of Zurich (Switzerland)
Instituto de Investigaciones Agropecuarias (Chile)
Lund University (Sweden)
Institute of Chinese Materia Medica (China)
More...
国外学术期刊发表的引用ChemFaces产品的部分文献
| 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. |
|
|
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 |
* Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
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