化合物BFH772 T3599

Product Introduction
Bioactivity


英文名: BFH772

描述: BFH772 是 VEGFR2抑制剂(IC50:3 nM)，具有口服活性。

细胞实验: 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)

激酶实验: 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].

体外活性: 每天口服3 mg/kgBFH772有效地抑制黑色素瘤的生长（原发性肿瘤减少54-90%;转移瘤减少71-96%）.

体内活性: BFH772抑制配体所诱导的RET、PDGFR、KIT激酶的自磷酸化,IC50为30-160 nM。BFH772有效地靶向VEGFR2,IC50为3 nM。而对FLK-1、FLT-1、FLT-4的有效性比对VEGFR2低500倍。除了VEGFR2,它还能靶向B-RAF,RET和TIE-2,尽管对它们的有效性比对VEGFR2低40倍以上。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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)


关键字: BFH-772 | inhibit | VEGFR | BFH 722 | Vascular endothelial growth factor receptor | Inhibitor | BFH722 | BFH 772 | BFH772

相关产品: (E)-FeCP-oxindole | Sunitinib Malate | CGP77675 | ODM-203 | VEGFR-2-IN-31 | ZD-4190 | VEGFR2-IN-3 | Licoricidin | PKI-166 | TG 100572

相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Pancreatic Cancer Compound Library | Reprogramming Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途