Brigatinib (Synonyms: 布格替尼; AP-26113)

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摩爾計(jì)算器

Brigatinib (AP-26113) 是一種有效，選擇性的，具有口服活性的 ALK 抑制劑，IC₅₀ 值為 0.6 nM。Brigatinib 可用于非小細(xì)胞肺癌 (NSCLC) 的研究。

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Brigatinib Chemical Structure

CAS No. : 1197953-54-0

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規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in Ethanol	￥771	In-stock
1 mg	￥272	In-stock
5 mg	￥600	In-stock
10 mg	￥950	In-stock
50 mg	￥2850	In-stock
100 mg	￥4550	In-stock
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Customer Review

Other Forms of Brigatinib:

Brigatinib-¹³C₆ 詢價(jià)
Brigatinib-d3 詢價(jià)

MCE 顧客使用本產(chǎn)品發(fā)表的 26 篇科研文獻(xiàn)

•Cancer Discov. 2024 Sep 13:OF1-OF20. [Abstract]
•Cancer Discov. 2018 Jun;8(6):714-729. [Abstract]
•Nat Cancer. 2022 Jun 20. [Abstract]
•Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. [Abstract]
•Nat Commun. 2024 Apr 23;15(1):3422. [Abstract]
•Cell Rep Med. 2023 Jan 10;100911. [Abstract]
•Theranostics. 2019 Jul 9;9(17):4878-4892. [Abstract]
•Pharmacol Res. 2018 Nov;137:47-55. [Abstract]
•J Med Chem. 2024 Oct 3. [Abstract]
•J Med Chem. 2024 Aug 8. [Abstract]
•Pharmaceutics. 2023 Sep 13, 15(9), 2312.
•iScience. 2023 Sep 22.

•Neoplasia. 2023 May 14;42:100908. [Abstract]
•Cancers (Basel). 2022, 14(1), 151.
•Spectrochim Acta A Mol Biomol Spectrosc. 2020 Nov 14;119210. [Abstract]
•Transl Oncol. 2021 Jan;14(1):100887. [Abstract]
•Clin Chim Acta. 2018 May;480:180-185. [Abstract]
•Mol Immunol. 2023 Mar 29;157:78-90. [Abstract]
•Fundam Clin Pharmacol. 2021 Feb 1. [Abstract]
•RSC Adv. 2018 8:1182-1190.
•ChemMedChem. 2017 Nov 22;12(22):1857-1865. [Abstract]
•Biomed Chromatogr. 2024 Oct;38(10):e5986. [Abstract]
•Biomed Chromatogr. 2023 Mar 20;e5628. [Abstract]
•Biol Pharm Bull. 45, 904-909 (2022).
•Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11. [Abstract]
•Maastricht University. 2023 Jun 1.

Brigatinib 相關(guān)產(chǎn)品

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生物活性
實(shí)驗(yàn)參考方法
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC₅₀ of 0.6 nM. Brigatinib can be used for research of NSCLC^[1].

IC₅₀ & Target

IC50: 0.6 nM (ALK)^[1]

細(xì)胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-431	IC₅₀	1.359 nM Compound: 6	Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
A-431	IC₅₀	709 nM Compound: Brigatinib	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay	[PMID: 35810715]
A-431	EC₅₀	936 nM Compound: 14	Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 37197473]
BaF3	IC₅₀	< 100 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring del19/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay Antiproliferative activity against mouse BaF3 cells harboring del19/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay	[PMID: 35810715]
BaF3	IC₅₀	0.155 μM Compound: 9	Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
BaF3	IC₅₀	0.17 μM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR 19del/T790M/C797S triple mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR 19del/T790M/C797S triple mutant after 72 hrs by CCK-8 assay	[PMID: 36279692]
BaF3	IC₅₀	0.26 μM Compound: 5	Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay	[PMID: 30429956]
BaF3	IC₅₀	0.286 μM Compound: 9	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
BaF3	IC₅₀	0.42 μM Compound: Brigatinib	Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay	[PMID: 31223440]
BaF3	IC₅₀	0.42 μM Compound: 5	Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay	[PMID: 30429956]
BaF3	IC₅₀	0.492 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 35446588]
BaF3	IC₅₀	0.56 μM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by CCK-8 assay	[PMID: 36279692]
BaF3	IC₅₀	0.61 μM Compound: 6	Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
BaF3	IC₅₀	1 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152P mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152P mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	1.91 μM Compound: 6	Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
BaF3	IC₅₀	10 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK V1180L mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK V1180L mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	10 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152R mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152R mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	12 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986Y mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986Y mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	19 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171T mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171T mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	20 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986F mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986F mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	EC₅₀	295 nM Compound: 14	Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 37197473]
BaF3	IC₅₀	35 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK T1151Tins mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK T1151Tins mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	35 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	36 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-D2033N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-D2033N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	39.9 nM Compound: 15	Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 33243531]
BaF3	IC₅₀	4.191 μM Compound: 9	Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
BaF3	IC₅₀	433 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring del18/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay Antiproliferative activity against mouse BaF3 cells harboring del18/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay	[PMID: 35810715]
BaF3	IC₅₀	47 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174V mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174V mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	48 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harbouring SLC34A2-ROS1-L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring SLC34A2-ROS1-L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	55.5 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring del19/T790M/C797S mutant assessed as inhibition of cell viability measured after 72 hrs by Celltiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring del19/T790M/C797S mutant assessed as inhibition of cell viability measured after 72 hrs by Celltiter-Glo assay	[PMID: 35413415]
BaF3	IC₅₀	67.2 nM Compound: 15	Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 33243531]
BaF3	IC₅₀	7.31 μM Compound: Brigatinib	Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay	[PMID: 31223440]
BaF3	IC₅₀	8.49 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells overexpressing ALK assessed as inhibition of cell proliferation measured by CCK8 assay Antiproliferative activity against mouse BaF3 cells overexpressing ALK assessed as inhibition of cell proliferation measured by CCK8 assay	[PMID: 34245852]
BaF3	IC₅₀	93 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171S mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171S mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	98 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174C mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174C mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
HEK-293T	IC₅₀	850 nM Compound: Brigatinib	Antiproliferative activity against human 293T cells overexpressing ALK G1202R mutant assessed as cell growth inhibition after 72 hrs Antiproliferative activity against human 293T cells overexpressing ALK G1202R mutant assessed as cell growth inhibition after 72 hrs	[PMID: 34138566]
KARPAS-299	GI₅₀	10 nM Compound: 11q; Brigatinib; AP26113	Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 27144831]
KARPAS-299	IC₅₀	29 nM Compound: 11q; Brigatinib; AP26113	Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 27144831]
LoVo	IC₅₀	2.03 μM Compound: 6	Inhibition of wild type EFGR expressed in human LoVo cell line assessed as inhibition of EGF-stimulated EGFR phosphorylation potency measured after 2 hrs by HRTF assay Inhibition of wild type EFGR expressed in human LoVo cell line assessed as inhibition of EGF-stimulated EGFR phosphorylation potency measured after 2 hrs by HRTF assay	[PMID: 34491761]
NCI-H1299	IC₅₀	1.049 μM Compound: 9	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay	[PMID: 35178175]
NCI-H1975	IC₅₀	0.62 μM Compound: Brigatinib	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay	[PMID: 31718182]
NCI-H1975	IC₅₀	0.64 μM Compound: Brigatinib	Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay	[PMID: 31718182]
NCI-H1975	IC₅₀	1.09 μM Compound: 5	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay	[PMID: 30429956]
NCI-H2228	IC₅₀	31.2 nM Compound: Brigatinib	Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell proliferation measured by CCK8 assay Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell proliferation measured by CCK8 assay	[PMID: 34245852]
NCI-H2228	IC₅₀	58.2 nM Compound: Brigatinib	Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 32179332]
PC-9	IC₅₀	0.829 μM Compound: 9	Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
PC-9	IC₅₀	1.11 μM Compound: 9	Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
PC-9	IC₅₀	1.454 nM Compound: 6	Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
PC-9	IC₅₀	599.2 nM Compound: Brigatinib	Antiproliferative activity against human PC-9 cells harboring EGFR del19/T790M/C797S mutant assessed as inhibition of cell viability measured after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human PC-9 cells harboring EGFR del19/T790M/C797S mutant assessed as inhibition of cell viability measured after 72 hrs by Celltiter-Glo assay	[PMID: 35413415]
Sf9	IC₅₀	0.001 μM Compound: Brigatinib	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k	[PMID: 31718182]
Sf9	IC₅₀	0.001 μM Compound: Brigatinib	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki	[PMID: 31718182]
Sf9	IC₅₀	0.13 μM Compound: Brigatinib	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay	[PMID: 31718182]
Sf9	IC₅₀	3 nM Compound: 3	Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA	[PMID: 31298540]
SR	IC₅₀	3.3 nM Compound: Brigatinib	Antiproliferative activity against human SR cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human SR cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 34138566]
U-937	IC₅₀	3194 nM Compound: 11q; Brigatinib; AP26113	Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 27144831]

體外研究
(In Vitro)

Brigatinib 能有效抑制 ALK（IC₅₀，0.6 nM）以及所有五種測(cè)試的突變變體（包括 G1202R（IC₅₀，0.6-6.6 nM））的體外激酶活性。
Brigatinib 表現(xiàn)出高度選擇性，僅抑制 11 種額外的天然或突變激酶，IC₅₀ <10 nM。這些包括 ROS1、FLT3 和 FLT3 (D835Y) 和 EGFR (L858R；IC₅₀，1.5-2.1 nM) 的突變變體。
Brigatinib 對(duì)具有 T790M 抗性突變（L858R/T790M）的 EGFR、天然 EGFR、IGF1R 和 INSR（IC₅₀，29-160 nM）表現(xiàn)出較溫和的活性，并且不抑制 MET（IC₅₀ >1000 nM）。
在細(xì)胞測(cè)定中，Brigatinib 抑制 ALK 和 ROS1，IC₅₀分別為 14 和 18 nM。
Brigatinib 抑制 FLT3 和 IGF-1R 的效力約降低 11 倍（IC₅₀，148-158 nM），抑制 FLT3 和 EGFR 的突變變體的效力降低 15 至 35 倍（IC₅₀，211-489 nM）。
Brigatinib 在三種 ALK 陰性 ALCL 和 NSCLC 細(xì)胞系中抑制細(xì)胞生長(zhǎng)，GI₅₀ 值范圍為 503 至 2,387 nM^[1]。
Brigatinib 抑制 ALK 活性并消除 ALK 成癮神經(jīng)母細(xì)胞瘤細(xì)胞系的增殖，IC₅₀ 為 75.27 ± 8.89 nM。
Brigatinib 分別在 10 nM 和 4 nM 水平上抑制 ALK-I1171N 和 ALK-G1269A 突變受體^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

體內(nèi)研究
(In Vivo)

Brigatinib（10、25 或 50 mg/kg，每日一次，口服）可導(dǎo)致 ALK⁺ Karpas-299 (ALCL) 和 H2228 (NSCLC) 異種移植小鼠模型中腫瘤生長(zhǎng)的劑量依賴性抑制。與 PF-02341066 相比，Brigatinib 可顯著提高 ALK⁺ 腦瘤小鼠的生存率^[1]。
Brigatinib（10、25、50 mg/kg，口服）具有劑量依賴性抗腫瘤活性，在 NSCLC 小鼠模型中導(dǎo)致腫瘤消退^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

584.09

Formula

C₂₉H₃₉ClN₇O₂P

CAS 號(hào)

1197953-54-0

性狀

固體

顏色

White to light yellow

中文名稱

布格替尼

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

Ethanol 中的溶解度 : 10 mg/mL (17.12 mM; 超聲加熱助溶)

DMSO 中的溶解度 : 2 mg/mL (3.42 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	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

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (1.71 mM); 澄清溶液

此方案可獲得 ≥ 1 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 10.0 mg/mL 的澄清 EtOH 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請(qǐng)依序添加每種溶劑： 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (1.71 mM); 澄清溶液

此方案可獲得 ≥ 1 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 10.0 mg/mL 的澄清 EtOH 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請(qǐng)依序添加每種溶劑： 10% EtOH 90% Corn Oil
Solubility: ≥ 1 mg/mL (1.71 mM); 澄清溶液

此方案可獲得 ≥ 1 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 10.0 mg/mL 的澄清 EtOH 儲(chǔ)備液加到 900 μL 玉米油中，混合均勻。
方案四

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.5 mg/mL (0.86 mM); 澄清溶液

此方案可獲得 ≥ 0.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 5.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案五

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.5 mg/mL (0.86 mM); 澄清溶液

此方案可獲得 ≥ 0.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 5.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案六

請(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 0.5 mg/mL (0.86 mM); 澄清溶液

此方案可獲得 ≥ 0.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 5.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購(gòu)。，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.98%

選擇批次：

Data Sheet (650 KB) SDS (615 KB)

COA (285 KB) LCMS (107 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Zhang S, et al. The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models. Clin Cancer Res. 2016 Nov 15;22(22):5527-5538 [Content Brief]

[2]. Huang WS, et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016 May 26;59(10):4948-64. [Content Brief]

[3]. Siaw JT, et al. Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice. Oncotarget. 2016 May 17;7(20):29011-22 [Content Brief]

Kinase Assay ^[1]	In vitro HotSpot^SM kinase profiling of 289 kinases is performed. The assay is conducted in the presence of 10 μM [³³P]-ATP, using brigatinib concentrations ranging from 0.05 nM to 1 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[3]	Cells are seeded at 15,000 per well with serial dilutions of the indicated inhibitors. After 72 hours cell viability is assessed by resazurin. IC₅₀ values are calculated with GraphPad Prism 6.0 by fitting data to a log (inhibitor concentration) vs. normalized response (variable slope) equation. Each experiment is performed in duplicate and repeated at least three times. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice: (1) Eight- to 10-week-old female SCID/beige mice are injected intravenously with 5×10⁶?H3122 cells per mouse and are randomly selected into treatment groups (n=10) when the average tumor size reaches appr 300 mm³ (day zero). Treatments are administered orally for up to 21 consecutive days at a 10 mL/kg dose volume. Subcutaneous tumors are measured two or three times weekly. Tumor volume (in mm³) is calculated using the formula (L×W²)/2. When a tumor reaches 10% of the body weight of the host, the animal is euthanized via CO₂ asphyxiation. (2) Eight- to 10-week old female SCID/beige mice are injected subcutaneously with 2.5×10⁶?Karpas-299 cells per mouse and are randomly selected into treatment groups (n=10) when the average tumor size reached appr 180 mm³ (day zero). Treatments are administered orally for 14 consecutive days at a 10 mL/kg dose volume. Tumor volume is measured and calculated as described for the H3122 model. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)	[1]. Zhang S, et al. The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models. Clin Cancer Res. 2016 Nov 15;22(22):5527-5538 [Content Brief] [2]. Huang WS, et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016 May 26;59(10):4948-64. [Content Brief] [3]. Siaw JT, et al. Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice. Oncotarget. 2016 May 17;7(20):29011-22 [Content Brief]

Brigatinib 相關(guān)分類

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO / Ethanol	1 mM	1.7121 mL	8.5603 mL	17.1206 mL	42.8016 mL
Ethanol	5 mM	0.3424 mL	1.7121 mL	3.4241 mL	8.5603 mL
	10 mM	0.1712 mL	0.8560 mL	1.7121 mL	4.2802 mL
	15 mM	0.1141 mL	0.5707 mL	1.1414 mL	2.8534 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Brigatinib1197953-54-0AP-26113布格替尼AP26113AP 26113Anaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246NSCLCcancerALK mutationInhibitorinhibitorinhibit

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Brigatinib (Synonyms: 布格替尼; AP-26113)

Customer Review

Other Forms of Brigatinib:

MCE 顧客使用本產(chǎn)品發(fā)表的 26 篇科研文獻(xiàn)

Brigatinib 相關(guān)產(chǎn)品

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純度 & 產(chǎn)品資料

參考文獻(xiàn)

摩爾計(jì)算器

稀釋計(jì)算器

Brigatinib 相關(guān)分類

完整儲(chǔ)備液配制表

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Brigatinib (Synonyms: 布格替尼; AP-26113)

Customer Review

Other Forms of Brigatinib:

Brigatinib 相關(guān)抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 26 篇科研文獻(xiàn)

Brigatinib 相關(guān)產(chǎn)品

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Brigatinib 相關(guān)抗體:

摩爾計(jì)算器

稀釋計(jì)算器

Brigatinib 相關(guān)分類

完整儲(chǔ)備液配制表

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