Research Area
Product Type
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TAE684 (NVP-TAE684) Chemical Structure
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Biological Activity
TAE684 (NVP-TAE684) is a highly potent and selective smallmolecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM. [1]
NVP-TAE684 treatment resulted in a rapid and sustained inhibition of phosphorylation of NPM-ALK and its downstream effectors and subsequent induction of apoptosis and cell cycle arrest. [1]
In vivo, NVP-TAE684 suppressed lymphomagenesis in two independent models of ALK-positive ALCL and induced regression of established Karpas-299 lymphomas. [1]
References on TAE684 (NVP-TAE684)
- [1] PNAS January 2, 2007;104:270–275
Chemical Information
| Molecular Weight (WM): | 614.2 |
|---|---|
| Formula: | C30H40ClN7O3S |
| CAS No.: | 761439-42-3 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥30mg/mL |
| Water <1mg/mL | |
| Ethanol ≥2mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Receptor Tyrosine Kinase >> ALK >> ALK Inhibitors
Angiogenesis >> ALK >> ALK Inhibitors
TGF-beta / smad >> ALK >> ALK Inhibitors
Angiogenesis >> ALK >> ALK Inhibitors
TGF-beta / smad >> ALK >> ALK Inhibitors
Notes:
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Selleck's high quality products have been used in several published research findings, including the following:
Using Tandem Mass Spectrometry in Targeted Mode to Identify Activators of Class IA PI3K in Cancer
Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinase inhibitors
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(A) H3122 xenografts harboring the EML4-ALK translocation were treated with control vehicle or the ALK inhibitor, TAE-684, for 2 days; the tumors were excised and lysates were prepared. The TIMM results for the control and treated animals are shown. (B) H3122 cells were treated in the presence or absence of TAE-684 (100 nM) for 6 hours in the presence or absence of the indicated ligands [EGF (50 ng/mL), IGF1 (50 ng/mL), and HGF (50 ng/mL)]. Extracts were probed with the indicated antibodies. - (A) H3122 xenografts harboring the EML4-ALK translocation were treated with control vehicle or the ALK inhibitor, TAE-684, for 2 days; the tumors were excised and lysates were prepared. The TIMM results for the control and treated animals are shown. (B) H3122 cells were treated in the presence or absence of TAE-684 (100 nM) for 6 hours in the presence or absence of the indicated ligands [EGF (50 ng/mL), IGF1 (50 ng/mL), and HGF (50 ng/mL)]. Extracts were probed with the indicated antibodies.
Data from [Cancer Res 2011 July;71:4920-31] TAE684 (NVP-TAE684) purchased from Selleck
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| (A) H3122 xenografts harboring the EML4-ALK translocation were treated with control vehicle or the ALK inhibitor, TAE-684, for 2 days; the tumors were excised and lysates were prepared. The TIMM results for the control and treated animals are shown. (B) H3122 cells were treated in the presence or absence of TAE-684 (100 nM) for 6 hours in the presence or absence of the indicated ligands [EGF (50 ng/mL), IGF1 (50 ng/mL), and HGF (50 ng/mL)]. Extracts were probed with the indicated antibodies. |
Data from [Cancer Res 2011 July;71:4920-31]
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