ASP3026 (Synonyms: ASP 3026;ASP-3026) |
Catalog No.GC14446
One-Click Copy Product Info
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An ALK inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1097917-15-1
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 1097917-15-1 | 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 | ≥ 14.5 mg/mL in DMSO, ≥ 4.9 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7219 mL | 8.6097 mL | 17.2194 mL |
| 5 mM | 344.4 μL | 1.7219 mL | 3.4439 mL |
| 10 mM | 172.2 μL | 861 μL | 1.7219 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)