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ASP3026ALK inhibitor,potent and selective

ASP3026

Catalog No. A3193
Size Price Stock Qty
5mg $70.00 In stock
10mg $100.00 In stock
50mg $300.00 In stock
200mg $700.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & MSDS

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Chemical structure

ASP3026

Biological Activity

Description ASP3026 is a selective inhibitor of ALK with IC50 value of 3.5 nM.
Targets ALK          
IC50 3.5 nM          

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Chemical Properties

Cas No. 1097917-15-1 SDF Download SDF
Synonyms ASP 3026;ASP-3026
Chemical Name 2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)-1,3,5-triazine-2,4-diamine
Canonical SMILES CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC=NC(=N2)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC
Formula C29H40N8O3S M.Wt 580.74
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

ASP3026 is a selective inhibitor of ALK with IC50 value of 3.5 nM [1].

ASP3026 is a potent ALK inhibitor and has a different selectivity with the reported ALK inhibitor crizotinib. When tested with a panel of 86 tyrosine kinases, ASP3026 showed the highest selectivity for ALK, ROS and ACK kinases. In NCI-H2228 NSCLC cells expressing EML4-ALK, five-day treatment of ASP3026 resulted in a cell growth inhibition with IC50 value of 64.8 nM. ASP3026 also inhibited the viability of NPM-ALK+ ALCL cells with IC50 values of 0.4, 0.75, 1 and 2.5 µM in SU-DHL-1, SUP-M2, SR-786 and Karpas 299 cells, respectively [2, 3].

In mouse model with NCI-H2228 subcutaneous xenograft, oral administration of ASP3026 caused significant reduction of phosphorylated ALK and tumor growth. 30 mg/kg/d ASP3026 for 2 weeks induced tumor regression by 78%. In mice injected with Karpas 299 cells, ASP3026 treatment caused remarkable lymphoma regression [2, 3].

References:
[1] Kuromitsu S, Mori M, Shimada I, et al. Anti-tumor activity of ASP3026, a novel and selective ALK inhibitor of anaplastic lymphoma kinase (ALK).Annual Meeting of the American Association for Cancer Research (AACR), Orlando, FL. 2011.
[2] Mori M, Ueno Y, Konagai S, et al. The Selective Anaplastic Lymphoma Receptor Tyrosine Kinase Inhibitor ASP3026 Induces Tumor Regression and Prolongs Survival in Non–Small Cell Lung Cancer Model Mice. Molecular cancer therapeutics, 2014, 13(2): 329-340.
[3] George S K, Vishwamitra D, Manshouri R, et al. The ALK inhibitor ASP3026 eradicates NPM-ALK+ T-cell anaplastic large-cell lymphoma in vitro and in a systemic xenograft lymphoma model. Oncotarget, 2014, 5(14): 5750-5763.