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Home
Angiogenesis
ALK inhibitor
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FLT3 inhibitor
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EGFR inhibitor
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ROS1 inhibitor
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IGF-1R inhibitor
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FLT inhibitor
Brigatinib
僅限科研使用
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
CAS: 1197953-54-0
產(chǎn)品質(zhì)控
批次：
純度：
99.91%
99.91
Brigatinib相關(guān)產(chǎn)品
| 相關(guān)產(chǎn)品 | TAE684 (NVP-TAE684) GSK1838705A Repotrectinib (TPX-0005) AZD3463 AP26113-analog (ALK-IN-1) ASP3026 Ensartinib dihydrochloride | 點(diǎn)擊展開(kāi) |
|---|---|---|
| 相關(guān)化合物庫(kù) | 酪氨酸激酶抑制劑分子庫(kù) PI3K/Akt 抑制劑庫(kù) 血管生成相關(guān)化合物庫(kù) HIF-1信號(hào)通路化合物庫(kù) FDA抗癌藥物庫(kù) | 點(diǎn)擊展開(kāi) |
相關(guān)信號(hào)通路圖
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。 | |||||||||||
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| 靶點(diǎn) |
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| 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[1]。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[2]。 | |||||
|---|---|---|---|---|---|---|
| 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。 |
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| 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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