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

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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

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Nature.
2017 Jan 19;541(7637):417-420.

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

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2016 Aug 5;353(6299)594-8

Nature Biotechnology.
2017 Jun;35(6):569-576

Cell.
2017 Jul 13;170(2):312-323

Cell.
2017 Apr 6;169(2):286-300.

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

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

Nature Medicine.
2017 Apr;23(4):493-500.

Cancer Cell.
2017 May 8;31(5):635-652.e6.

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

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

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2017 Jun;18(6):654-664.

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

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2016 Sep;26(9):1007-20.

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2017 May 18;66(4):546-557.

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2016 Feb 1;7:10492.

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

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2015 Jun 30;112(26):E3365-73.

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2015 Jul 28;112(30):9412-7.

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

Cancer Res canres.
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2016 Jan 14;5. pii: e12203.

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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.

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

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Quality Control

Quality Control & MSDS

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Purity = 98.00%

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

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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	>26.5mg/mL in DMSO	Storage	Store at -20°C
General tips	N/A
Shipping Condition	N/A

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.