AP26113 (Brigatinib)

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ALK inhibitor

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Catalog No. A11948

Availability:Stock in USAIn stock

Product Name Catalog No. Price Qty
AP26113 5mg A11948-5

Regular Price: $90.00

Special Price: $76.50

AP26113 10mg A11948-10

Regular Price: $140.00

Special Price: $119.00

AP26113 25mg A11948-25

Regular Price: $220.00

Special Price: $187.00

AP26113 50mg A11948-50

Regular Price: $320.00

Special Price: $272.00

AP26113 10mM * 1mL in DMSO A11948-10mM-D

Regular Price: $120.00

Special Price: $102.00

Products are for laboratory research use only. Not for human use. We do not sell to patients.

Quick Overview

AP26113 is an orally-available, potent, and selective inhibitor of ALK with a potency of 0.62 nM against wild-type and activity against a wide range of mutants, including the crizotinib-resistant L1196M line. In a panel of EML4-ALK or NPM-ALK-positive cell lines, AP26113 has IC50 values of 4-31 nM. [1][2]
AP26113 is effective against sensitive and resistant H3122 cells, reducing cell growth, suppressing ALK phosphorylation, and inducing apoptosis. In Ba/F3 cells expressing native or mutant EML4-ALK, AP26113 was active at IC50s of 10 and 24 nM, respectively. [3]

AP26113 (Brigatinib)

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Chemical Information

Catalog Num A11948
Actions Inhibitor
M. Wt 529.01
Formula C26H34ClN6O2P
Solubility DMSO
Purity >98%
Storage at -20°C 2 years
CAS No. 1197958-12-5
Synonyms AP-26113
SMILES code CN(C)C1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC=CC=C4P(=O)(C)C)Cl)OC
Chemical Name (2-((5-chloro-2-((4-(4-(dimethylamino)piperidin-1-yl)-2-methoxyphenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide

Biological Activity

Description
AP26113 is an orally-available, potent, and selective inhibitor of ALK with a potency of 0.62 nM against wild-type and activity against a wide range of mutants, including the crizotinib-resistant L1196M line. In a panel of EML4-ALK or NPM-ALK-positive cell lines, AP26113 has IC50 values of 4-31 nM. [1][2] AP26113 is effective against sensitive and resistant H3122 cells, reducing cell growth, suppressing ALK phosphorylation, and inducing apoptosis. In Ba/F3 cells expressing native or mutant EML4-ALK, AP26113 was active at IC50s of 10 and 24 nM, respectively. [3]
Targets
Target Value
ALKIC50: 0.62nM
FERIC50: 1.3nM
ROS/ROS1IC50: 1.9nM
FLT3IC50: 2.1nM
FES/FPSIC50: 3.4nM
FAK/PTK2IC50: 3.8nM
BRKIC50: 4.1nM
STK22DIC50: 4.3nM
Chk2IC50: 6.5nM
RSK2IC50: 13nM
TYK/LTKIC50: 13nM
YESIC50: 19nM
PYK2IC50: 24nM
ErbB4IC50: 27nM
CLK1IC50: 29nM
CaMKIIdIC50: 29nM
Chk1IC50: 30nM
RSK1IC50: 30nM
RSK4IC50: 42nM
IRR/INSRRIC50: 45nM
IGF-1RIC50: 46nM
ARK5IC50: 47nM
CaMKIIgIC50: 48nM
LRRK2IC50: 51nM
FRKIC50: 52nM
FLT4IC50: 58nM
RETIC50: 65nM
CaMKK2IC50: 83nM
MARK2IC50: 94nM
PKCnuIC50: 95nM
PHKg2IC50: 108nM
LOK/STK10IC50: 123nM
BRSK2IC50: 125nM
MARK3IC50: 127nM
MARK1IC50: 127nM
FGFR1IC50: 128nM
EGFRIC50: 129nM
BLKIC50: 136nM
TSSK2IC50: 138nM
AuroraAIC50: 146nM
JAK2IC50: 154nM
FGFR4IC50: 181nM
PKCmu/PKD1IC50: 197nM
FynIC50: 198nM
HckIC50: 198nM
MLK1/MAP3K9IC50: 218nM
FGFR2IC50: 228nM
CLK2IC50: 240nM
LynIC50: 241nM
PKD2/PRKD2IC50: 285nM
c-SrcIC50: 329nM
BRSK1IC50: 338nM
FGFR3IC50: 358nM
FmsIC50: 358nM
Insulin ReceptorIC50: 395nM
SIK2/SNF1LK2/QIKIC50: 466nM
FGRIC50: 491nM
TAOK1IC50: 492nM
Abl1IC50: 500nM
LCKIC50: 512nM
PLK1IC50: 611nM
BTKIC50: 673nM[null]

Solubility

Solubility (25°C) * In vitro DMSO 45 mg/mL (85.06 mM)
Water <1 mg/mL (<1 mM)
Ethanol 106 mg/mL (200.37 mM)
In vivo NMP/polyethylene glycol 300 (10/90, v/v) 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

General References

1.  Shiao et al., Anaplastic Lymphoma Kinase (ALK) Inhibitors: New Cancer Breakthroughs for Lung Cancer, J. Cancer. Res. Pract. 2011, 27(4), 143-156.
2.  Rivera et al., Efficacy and pharmacodynamic analysis of AP26113, a potent and selective orally active inhibitor of Anaplastic Lymphoma Kinase (ALK). Cancer Res. 2010, 70(8), Suppl 1., AACR 101st Annual Meeting 2010.
3.  Katayama et al., Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc. Natl. Acad. Sci. 2011, 108(18), 7535-7540. Pubmed ID: 21502504

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