[CAS NO. 1197953-54-0] Brigatinib (AP26113)

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PRODUCTS SPECIFICATIONS [1197953-54-0]

Catalog

SLK-S8229

Brand

Selleck

CAS

1197953-54-0

DESCRIPTION [1197953-54-0]

Overview

MDL	MFCD29472221
Molecular Weight	584.09
Molecular Formula	C29H39ClN7O2P
SMILES	CN1CCN(C2CCN(C3=CC=C(NC4=NC=C(Cl)C(NC5=CC=CC=C5P(C)(C)=O)=N4)C(OC)=C3)CC2)CC1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.7121 mL	8.5603 mL	17.1206 mL
5 mM	0.3424 mL	1.7121 mL	3.4241 mL
10 mM	0.1712 mL	0.8560 mL	1.7121 mL
50 mM	0.0342 mL	0.1712 mL	0.3424 mL

Description

Brigatinib (AP26113) is a potent and selective (IC50, 0.6 nM) and (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.

Targets

In vitro

Beyond ALK, IGF1R, and InsR, brigatinib also potently inhibits FLT3 and ROS1 with IC50 values of 2.1 and 1.9 nM, respectively. It does not show significant activity toward c-Met or Ron up to 1 μM. Brigatinib overcomes the resistance of EGFR-triple-mutant and the activity depends on ATP-competitive manner with less affection to wild-type EGFR.

In vivo

Mouse PK parameters for Brigatinib following oral dosing (10 mg/kg): C=448 ng/mL,t=5.8 h. And in CD rats, after dosing at 3 mg/kg i.v, CL=0.46 L/(h·kg), t=4.8 h, Vss=7.8 L/kg; Dosed at 10 mg/kg p.o, Cmax=305 ng/mL, t=4 h, t=3.4 h， F%=52. Brigatinib demonstrates dose-dependent antitumor activity. Brigatinib demonstrates growth inhibition activity in PC9 triple-mutant xenograft model and in combination with anti-EGFR antibody to potentiate the efficacy both in vitro and in vivo as shown in first-generation EGFR-TKI-resistant patients.

References

[1] Wei-Sheng Huang, et al. J Med Chem, 2016, 59(10):4948-4964.
[2] Uchibori, K et al. Nat. Commun. 8, 14768 doi: 10.1038/ncomms14768 (2017).