AP26113|Anaplastic lymphoma kinase (ALK) inhibitor|CAS# 1197958-12-5

Home >> Signaling Pathways >> JAK/STAT Signaling >> EGFR >> AP26113

Size	Price	Stock
10mM (in 1mL DMSO)	$125.00	In stock
Evaluation Sample	$28.00	In stock
5mg	$100.00	In stock
10mg	$150.00	In stock
50mg	$350.00	In stock
100mg	$450.00	In stock

Publications citing ApexBio Products

Nature.
2016 Apr 21;532(7599):398-401.

Nature.
2015 Aug 20;524(7565):309-14.

Cell.
2015 Aug 27;162(5):987-1002.

Cell.
2015 Feb 12;160(4):729-44.

Immunity.
2016 Jan 19;44(1):88-102

Nat Cell Biol.
2015 May;17(5):627-38.

Nat Neurosci.
2015 Oct;18(10):1464-73.

Nat Commun.
2016 Feb 1;7:10492.

J Cell Biol.
2016 Apr 11;213(1):109-25.

Cell Host Microbe.
2016 Jul 13;20(1):13-24.

Proc Natl Acad Sci U S A.
2016 Mar 8;113(10):2585-90.

Proc Natl Acad Sci U S A.
2015 Jun 30;112(26):E3365-73.

Proc Natl Acad Sci U S A.
2015 Jul 28;112(30):9412-7.

Autophagy.
2016 Jul 2;12(7):1129-52.

Cancer Res canres.
2946.2015.

Elife.
2016 Jan 14;5. pii: e12203.

Nucleic Acids Res.
2016 Feb 18;44(3):e2.

EMBO Rep.
2015 Sep;16(9):1114-30.

Oncogene.
2016 Mar 21.

Cell Rep.
2015 Sep 29;12(12):1986-96.

Cell Death Differ.
2016 Jun;23(6):1026-37.

Cell Death Differ.
2016 Jan;23(1):76-88.

Diabetes Obes Metab.
2015 Apr;17(4):403-13.

Oncotarget.
2015 Jan 20;6(2):1171-89.

J Neurosci.
2015 Sep 23;35(38):13244-56.

Sci Signal.
2014 Dec 23;7(357):ra122.

Mol Ther.
2015 Sep;23(9):1475-85.

J Nucl Med.
2016 Feb;57 Suppl 1:75S-80S.

Cardiovasc Res.
2015 Apr 1;106(1):153-62.

Cell Mol Life Sci.
2015 Nov;72(22):4399-407.

Anal Chem.
2015;87(10):5046-9.

Cancer Lett.
2016 Apr 28;374(1):1-11.

Quality Control

Quality Control & MSDS

View current batch:

Purity = 98.00%

COA (Certificate Of Analysis)
MSDS (Material Safety Data Sheet)

Chemical structure

Related Biological Data

Biological Activity

Description	AP26113 is a potent inhibitor of ALK with IC50 of 0.62 nM.
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

calculate

AP26113 Molarity Calculator

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 > 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

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.