ASP 3026

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Cat.No. 5310 - ASP 3026 | C29H40N8O3S | CAS No. 1097917-15-1
Description: Potent anaplastic lymphoma kinase (ALK) inhibitor; also potent ACK inhibitor
Chemical Name: N2-[2-Methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-1,3,5-triazine-2,4-diamine
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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.

Compound Libraries

ASP 3026 is also offered as part of the Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 11.61 20

Preparing Stock Solutions

The following data is based on the product molecular weight 580.74. Batch specific molecular weights may vary from batch to batch due to solvent 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

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References

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


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Citations for ASP 3026

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