Search Site
Related Biochemicals Related Antibodies

AP26113

Dual inhibitor of anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR).

AP26113

Catalog No. A1367
Size Price Stock Qty
5mg $150.00 In stock
Evaluation Sample $28.00  All Inclusive In stock
25mg $480.00 In stock
100mg $1,000.00 In stock

All inclusive: Shipping and all other fees included

Tel: +1-832-696-8203

Email: sales@apexbt.com

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

AP26113

Biological Activity

Targets ALK FER ROS/ROS1 FLT3 FES/FPS  
IC50 0.62 nM 1.3 nM 1.9 nM 2.1 nM 3.4 nM  

AP26113 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

AP26113 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 1197958-12-5 SDF Download SDF
Chemical Name 5-chloro-2-N-[4-[4-(dimethylamino)piperidin-1-yl]-2-methoxyphenyl]-4-N-(2-dimethylphosphorylphenyl)pyrimidine-2,4-diamine
Canonical SMILES CN(C)C1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC=CC=C4P(=O)(C)C)Cl)OC
Formula C26H34ClN6O2P M.Wt 529.01
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

AP26113 is a novel, synthetic, orally available small-molecule inhibitor of anaplastic lymphoma kinase (ALK), which is a receptor tyrosine kinase in the insulin receptor superfamily, with half maximal inhibitory concentration IC50 ranging from 5 nmol/l to 11 nmol/l. AP26113 is also capable of inhibiting the ALK tyrosine kinase gatekeeper mutation L1196M (IC50: 15 nmol/l to 45 nmol/L), mutant epidermal growth factor receptor (EGFR) containing the gatekeeper T790M mutation and c-ros oncogene 1 (ROS1). Moreover, AP26113 has been found to be active against H3122 cells (both sensitive and resistant) and Ba/F3 cells harboring native or mutant EML4-ALK (IC50: 10 nM and 24 nM respectively).

References:
[1]Solomon B, Wilner KD, Shaw AT. Current status of targeted therapy for anaplastic lymphoma kinase-rearranged non-small cell lung cancer. Clin Pharmacol Ther. 2014 Jan;95(1):15-23. doi: 10.1038/clpt.2013.200. Epub 2013 Oct 3.
[2]Katayama R1, Khan TM, Benes C, Lifshits E, Ebi H, Rivera VM, Shakespeare WC, Iafrate AJ, Engelman JA, Shaw AT. Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci U S A. 2011 May 3;108(18):7535-40. doi: 10.1073/pnas.1019559108. Epub 2011 Apr 18.