| 名稱 | BFH772 |
| 描述 | BFH772, a structure analogue of BAW2881, is a potent and selective VEGF inhibitor. BFH772 is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC50 values ranging between 30 and 160 nM. |
| 細(xì)胞實(shí)驗(yàn) | Subconfluent HUVECs were incubated in triplicate in 96-well plates with basal medium containing 1.5% FCS and a constant concentration of VEGF (10 ng/mL), bFGF (0.5 ng/mL), or FCS (5%) in the presence or absence of compounds. After 24 h of incubation, BrdUrd labeling solution was added and cells incubated an additional 24 h before fixation, blocking, and addition of peroxidaselabeled anti-BrdUrd antibody. Bound antibody was then detected spectrophotometrically at 450 nm.(Only for Reference) |
| 激酶實(shí)驗(yàn) | In vitro kinase assay is based on a filter binding assay, using the recombinant GST-fused kinase domains expressed in baculovirus and purified over glutathione-sepharose, γ-[33P]ATP as the phosphate donor, and poly(Glu:Tyr 4:1) peptide as the acceptor. Each GST-fused kinase is incubated under optimized buffer conditions [20 mM Tris-HCl buffer (pH 7.5), 1-3 mM MnCl2, 3-10 mM MgCl2, 3-8 μg/mL poly(Glu:Tyr 4:1), 0.25 mg/mL polyethylene glycol 20000, 8 μM ATP, 10 μM sodium vanadate, 1 mM DTT] and 0.2 μCi γ-33P ATP in a total volume of 30 μL in the presence or absence of a test substance for 10 min at ambient temperature. The reaction is stopped by adding 10 mL of 250 mM EDTA. Using a 384-well filter system, half the volume is transferred onto an Immobilon-polyvinylidene difluoride membrane. The membrane is then washed extensively and dried, and scintillation counting is performed. IC50s for compounds are calculated by linear regression analysis of the percentage inhibition[1]. |
| 體外活性 | 每天口服3 mg/kgBFH772有效地抑制黑色素瘤的生長(zhǎng)（原發(fā)性腫瘤減少54-90%;轉(zhuǎn)移瘤減少71-96%）. |
| 體內(nèi)活性 | BFH772抑制配體所誘導(dǎo)的RET、PDGFR、KIT激酶的自磷酸化,IC50為30-160 nM。BFH772有效地靶向VEGFR2,IC50為3 nM。而對(duì)FLK-1、FLT-1、FLT-4的有效性比對(duì)VEGFR2低500倍。除了VEGFR2,它還能靶向B-RAF,RET和TIE-2,盡管對(duì)它們的有效性比對(duì)VEGFR2低40倍以上。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : 81 mg/mL (184.3 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 81 mg/mL (184.3 mM)
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| 關(guān)鍵字 | BFH-772 | inhibit | VEGFR | BFH 722 | Vascular endothelial growth factor receptor | Inhibitor | BFH722 | BFH 772 | BFH772 |
| 相關(guān)產(chǎn)品 | Ribociclib | Lenvatinib | Axitinib | Sorafenib tosylate | Lenvatinib mesylate | Sanguinarine chloride | Regorafenib | Pazopanib | Nintedanib | Sorafenib | Regorafenib monohydrate | Taxifolin |
| 相關(guān)庫(kù) | 抑制劑庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | 激酶抑制劑庫(kù) | 膜蛋白靶向化合物庫(kù) | 酪氨酸激酶分子庫(kù) | 藥物功能重定位化合物庫(kù) | 抗癌臨床化合物庫(kù) | 抗癌藥物庫(kù) | 細(xì)胞重編程化合物庫(kù) |