Brigatinib | pan-ALK inhibitor

CAS:
1197953-54-0
Catalog Number:
10-5034
Activity:
pan-ALK inhibitor
Chemical Names:
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 (1 mg/ml with warming)
Physical Properties:
White to off-white solid
Purity:
98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$50.00
25 mg$160.00

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
CAS:
1197953-54-0
Catalog Number:
10-5034
Activity:
pan-ALK inhibitor
Chemical Names:
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 (1 mg/ml with warming)
Physical Properties:
White to off-white solid
Purity:
98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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