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Submit ReviewASP 3026 is a potent anaplastic lymphoma kinase (ALK) inhibitor (IC50 = 3.5 nM). Also inhibits Ack and ROS1 activity (IC50 values are 5.8 and 8.9 nM respectively). Attenuates proliferation, and induces apoptosis of NPM-ALK+ T cell anaplastic large-cell lymphoma (ALCL) cells in vitro. Suppresses tumor growth of NPM-ALK+ ALCL cell xenografts in mice. Causes tumor shrinkage in hEML4-ALK transgenic mice. Orally available.
ASP 3026 is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
M. Wt | 580.74 |
Formula | C29H40N8O3S |
Storage | Store at -20°C |
Purity | ≥99% (HPLC) |
CAS Number | 1097917-15-1 |
PubChem ID | 25134326 |
InChI Key | MGGBYMDAPCCKCT-UHFFFAOYSA-N |
Smiles | CN1CCN(C2CCN(C3=CC=C(NC4=NC(NC5=C(S(C(C)C)(=O)=O)C=CC=C5)=NC=N4)C(OC)=C3)CC2)CC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 11.61 | 20 |
The following data is based on the product molecular weight 580.74. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.2 mM | 8.61 mL | 43.05 mL | 86.1 mL |
1 mM | 1.72 mL | 8.61 mL | 17.22 mL |
2 mM | 0.86 mL | 4.3 mL | 8.61 mL |
10 mM | 0.17 mL | 0.86 mL | 1.72 mL |
References are publications that support the biological activity of the product.
George et al (2014) The ALK inhibitor ASP3026 eradicates NPM-ALK+ T-cell anaplastic large-cell lymphoma in vitro and in a systemic xenograft lymphoma model. Oncotarget 5 5750 PMID: 25026277
Awad and Shaw (2014) ALK Inhibitors in Non-Small Cell Lung Cancer: Crizotinib and Beyond. Clin.Adv.Hematol.Oncol. 12 429 PMID: 25322323
Mori et al (2014) The selective anaplastic lymphoma receptor tyrosine kinase inhibitor ASP3026 induces tumor regression and prolongs survival in non-small cell lung cancer model mice. Mol.Cancer Ther. 13 329 PMID: 24419060
If you know of a relevant reference for ASP 3026, please let us know.
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