Brigatinib

製品コードS8229 バッチS822901

印刷

化学情報

Synonyms

AP26113

Storage
(From the date of receipt)

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

化学式

C₂₉H₃₉ClN₇O₂P

分子量

584.09

CAS No.

1197953-54-0

Solubility (25°C)*

体外

Ethanol (warmed with 50ºC water bath)

2 mg/mL (3.42 mM)

DMSO (warmed with 50ºC water bath)

1 mg/mL (1.71 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Brigatinibは、強力で選択的なALK（IC50、0.6 nM）およびROS1（IC50、0.9 nM）阻害剤です。また、IGF-1R、FLT3、およびFLT3（D835Y）とEGFRの変異型をより低い効力で阻害します。
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. This compound 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_max=448 ng/mL,t_1/2=5.8 h. And in CD rats, after dosing at 3 mg/kg i.v, CL=0.46 L/(h·kg), t_1/2=4.8 h, Vss=7.8 L/kg; Dosed at 10 mg/kg p.o, Cmax=305 ng/mL, t_max=4 h, t_1/2=3.4 h， F%=52. This compound demonstrates dose-dependent antitumor activity. It 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.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	U937 cells, Karpas-299 cells, H3122 cells
	濃度	--
	反応時間	72 h
	実験の流れ	All cell lines were used within 20 passages of the initial thaw. Following inhibitor treatment for 72 h, cell growth was assessed to determine the concentration that causes 50% inhibition of cell viability (IC50).
動物実験	動物モデル	female CD rats
	投薬量	10 mg/kg(p.o); 2 mg/kg(i.v)
	投与方法	p.o, i.v

参考

http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.6b00306
https://www.nature.com/articles/ncomms14768

カスタマーフィードバック

: Data from [Data independently produced by , , Mol Cancer Res, 2017, 15(1):106-114]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Targeting proteostasis in multiple myeloma through inhibition of LTK [ Leukemia, 2025, 10.1038/s41375-025-02682-8]	PubMed: 40634511
Novel selective strategies targeting the BCL-2 family to enhance clinical efficacy in ALK-rearranged non-small cell lung cancer [ Cell Death Dis, 2025, 16(1):194]	PubMed: 40113795
Brigatinib activates inflammasomes: Implication for immune-related adverse events [ Toxicol Appl Pharmacol, 2025, 498:117310]	PubMed: 40122348
Preclinical Prediction of Resistance Mutations and Proposal of Sequential Treatment Strategies for ALK-positive Lung Cancer Using Next-generation ALK Inhibitors [ Pharm Res, 2025, 42(9):1497-1509]	PubMed: 40993323
KinoViz: A User-Friendly Web Application for High-Throughput Kinome Profiling Analysis and Visualization in Cancer Research [ Res Sq, 2025, rs.3.rs-6431257]	PubMed: 40630533
NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations [ Cancer Discov, 2024, OF1-OF20.]	PubMed: 39269178
LTK mutations responsible for resistance to lorlatinib in non-small cell lung cancer harboring CLIP1-LTK fusion [ Commun Biol, 2024, 7(1):412]	PubMed: 38575808
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271
Selective impact of ALK and MELK inhibition on ERα stability and cell proliferation in cell lines representing distinct molecular phenotypes of breast cancer [ Sci Rep, 2024, 14(1):8200]	PubMed: 38589728
Secondary Mutations of the EGFR Gene That Confer Resistance to Mobocertinib in EGFR Exon 20 Insertion [ J Thorac Oncol, 2023, S1556-0864(23)00797-9]	PubMed: 37666482

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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