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Product Details

Brigatinib | pan-ALK inhibitor

Brigatinib (1197953-54-0) is a potent and selective pan-ALK inhibitor IC50=0.6 nM.1 Cells with ALK mutation L1196Q2 and the double mutation I1171S + G12693 remain sensitive to brigatinib. Clinically useful in non-small cell lung cancer.4

References/Citations

1) Zhang et al. (2016), The potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models; Clin. Cancer Res., 22 5527
2) Ceccon et al. (2013), Crizotinib-resistant NPM-ALK mutants confer differential sensitivity to unrelated Alk inhibitors; Mol. Cancer Res., 11 122
3) Takahashi et al. (2020), Overcoming resistance by ALK compound mutation (I1171S + G1269A) after sequential treatment of multiple ALK inhibitors in non-small cell lung cancer; Thorac. Cancer., 11 581
4) Pinto et al. (2020), Clinical consequences of resistance to ALK inhibitors in non-small cell lung cancer; Respir. Med., 14 385

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Catalog#  10-5034-0005

$50.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
1197953-54-0
Catalog Number:
10-5034
Activity:
pan-ALK inhibitor
Chemical Name:
5-Chloro-N4-[2-(dimethylphosphinyl)phenyl]-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-2,4- pyrimidinediamine
Alternate name:
AP26113
Molecular Weight:
584.02
Molecular Formula:
C29H39ClN7O2P
Solubility:
Soluble in DMSO (up to 1 mg/ml with warming).
Physical Properties:
White or off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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