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Brigatinib

別名: AP26113 中文名稱：布格替尼,布加替尼

Brigatinib是一種有效的、選擇性的ALK抑制劑，IC50=0.6 nM；也是ROS1抑制劑，IC50=0.9 nM。它還能以相對(duì)較低的效力抑制IGF-1R、FLT3、FLT3(D835Y)和EGFR。

Brigatinib Chemical Structure

Brigatinib Chemical Structure

CAS: 1197953-54-0

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
5mg 759.19 現(xiàn)貨
25mg 2433.38 現(xiàn)貨
100mg 5544.76 現(xiàn)貨
1g 12039.3 現(xiàn)貨
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細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息(PMID)
KARPAS299 Antitumor assay 50 mg/kg 13 days Antitumor activity against human KARPAS299 cells expressing NMP-ALK fusion protein xenografted in SCID/beige mouse assessed as tumor regression at 50 mg/kg, po administered once daily for 13 days, NULL = NULL μM. 27144831
KARPAS299 Antiproliferative assay 72 hrs 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, GI50 = 0.01 μM. 27144831
KARPAS299 Antiproliferative assay 72 hrs 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, IC50 = 0.029 μM. 27144831
Ba/F3 Function assay 72 hrs Inhibition of human EGFR del19/T790M/C797S mutant expressed in mouse Ba/F3 cells assessed as cell growth inhibition after 72 hrs by CellTiter-Glo assay, GI50 = 0.0672 μM. 29136465
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay, IC50 = 0.26 μM. 30429956
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay, IC50 = 0.42 μM. 30429956
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay, IC50 = 1.09 μM. 30429956
U937 Antiproliferative assay 72 hrs 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, IC50 = 3.194 μM. 27144831
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述 Brigatinib是一種有效的、選擇性的ALK抑制劑，IC50=0.6 nM；也是ROS1抑制劑，IC50=0.9 nM。它還能以相對(duì)較低的效力抑制IGF-1R、FLT3、FLT3(D835Y)和EGFR。
靶點(diǎn)
ALK
(Cell-free assay)		 ROS1
(Cell-free assay)		 FLT3
(Cell-free assay)		 IGF1R
(Cell-free assay)		 EGFR(C797S/del19)
(cell-based)		 點(diǎn)擊更多
0.37 nM 1.9 nM 2.1 nM 24.9 nM 39.9 nM
體外研究(In Vitro)
體外研究活性 除了ALK, IGF1R和InsR，brigatinib也能有效地抑制FLT3和ROS1，IC50分別為2.1 nM和1.9 nM。在1 μM時(shí)，brigatinib對(duì)c-Met或Ron沒(méi)有顯著活性。Brigatinib可克服EGFR三突變體的耐藥性，這一活性依賴于ATP競(jìng)爭(zhēng)性，對(duì)野生型EGFR的影響較小。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 U937細(xì)胞, Karpas-299細(xì)胞, H3122細(xì)胞
濃度 --
孵育時(shí)間 72 h
方法

將細(xì)胞用抑制劑處理72小時(shí)，檢測(cè)細(xì)胞生長(zhǎng)情況，確定IC50值。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot

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