达沙替尼

Dasatinib (BMS-354825)

	产品编号	CFN60030
	CAS编号	302962-49-8
	分子式 = 分子量	C₂₂H₂₆ClN₇O₂S = 488.01
	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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达沙替尼	CFN60030	302962-49-8	1mg	QQ客服：215959384
达沙替尼	CFN60030	302962-49-8	5mg	QQ客服：215959384
达沙替尼	CFN60030	302962-49-8	10mg	QQ客服：215959384
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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

The Ohio State University (USA)

University of Vigo (Spain)

Lodz University of Technology (Poland)

Shanghai University of TCM (China)

University of Hertfordshire (United Kingdom)

National Cancer Center Research Institute (Japan)

University of Padjajaran (Indonesia)

Deutsches Krebsforschungszentrum (Germany)

University of Bonn (Germany)

Srinakharinwirot University (Thailand)

Universidad de Antioquia (Colombia)

University of Queensland (Australia)

University of Malaya (Malaysia)

National Cancer Institute (USA)

More...

Description:

Dasatinib (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.

Targets:

Abl | Src | c-Kit | Autophagy

In vitro:

Clin Cancer Res,2012 Jul 1;18(13):3580-91.

Targeted inhibition of Src kinase with dasatinib blocks thyroid cancer growth and metastasis.[Pubmed: 22586301]

There are no effective therapies for patients with poorly differentiated papillary thyroid cancer (PTC) or anaplastic thyroid cancer (ATC), and metastasis to the bone represents a significantly worse prognosis. Src family kinases (SFKs) are overexpressed and activated in numerous tumor types and have emerged as a promising therapeutic target, especially in relation to metastasis. We recently showed that Src is overexpressed and activated in thyroid cancer. We therefore tested whether inhibition of Src with dasatinib (BMS-354825) blocks thyroid cancer growth and metastasis.
METHODS AND RESULTS:
The effects of dasatinib on thyroid cancer growth, signaling, cell cycle, and apoptosis were evaluated in vitro. The therapeutic efficacy of dasatinib was further tested in vivo using an orthotopic and a novel experimental metastasis model. Expression and activation of SFKs in thyroid cancer cells was characterized, and selectivity of dasatinib was determined using an Src gatekeeper mutant. Dasatinib treatment inhibited Src signaling, decreased growth, and induced cell-cycle arrest and apoptosis in a subset of thyroid cancer cells. Immunoblotting showed that c-Src and Lyn are expressed in thyroid cancer cells and that c-Src is the predominant SFK activated. Treatment with dasatinib blocked PTC tumor growth in an orthotopic model by more than 90% (P = 0.0014). Adjuvant and posttreatment approaches with dasatinib significantly inhibited metastasis (P = 0.016 and P = 0.004, respectively).
CONCLUSIONS:
These data provide the first evidence that Src is a central mediator of thyroid cancer growth and metastasis, indicating that Src inhibitors may have a higher therapeutic efficacy in thyroid cancer, as both antitumor and antimetastatic agents.

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	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	2.0491 mL	10.2457 mL	20.4914 mL	40.9828 mL	51.2285 mL
5 mM	0.4098 mL	2.0491 mL	4.0983 mL	8.1966 mL	10.2457 mL
10 mM	0.2049 mL	1.0246 mL	2.0491 mL	4.0983 mL	5.1228 mL
50 mM	0.041 mL	0.2049 mL	0.4098 mL	0.8197 mL	1.0246 mL
100 mM	0.0205 mL	0.1025 mL	0.2049 mL	0.4098 mL	0.5123 mL