Brigatinib

製品コードS8229 バッチS822904

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)

5 mg/mL (8.56 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.
Clear solution	50%DMSO 1 50%Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.750mg/ml (1.28mM)	Taking the 1 mL working solution as an example, add 500 μL of 1.5 mg/ml clear DMSO stock solution to 500 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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 is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.
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^[1]. This compound overcomes the resistance of EGFR-triple-mutant and the activity depends on ATP-competitive manner with less affection to wild-type EGFR^[2].
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^[1]. 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^[2].

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
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
Adaptive resistance to lorlatinib via EGFR signaling in ALK-rearranged lung cancer [ NPJ Precis Oncol, 2023, 7(1):12]	PubMed: 36702855
Adaptive resistance to lorlatinib via EGFR signaling in ALK-rearranged lung cancer [ NPJ Precis Oncol, 2023, 7(1):12]	PubMed: 36702855

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。