Powder: -20°C for 3 years | In solvent: -80°C for 1 year
OSI-930 是 Kit,KDR 和 CSF-1R (c-Fms)的口服选择性抑制剂,IC50分别为 80 nM,9 nM 和 15 nM。它具有抗肿瘤活性,靶向肿瘤中的癌细胞增殖和血管生成。它还适度抑制 Flt-1,c-Raf 和 Lck,并且对 PDGFRα/β,Flt-3和 Abl 具有较弱的抑制活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 328 | 现货 | ||
2 mg | ¥ 455 | 现货 | ||
5 mg | ¥ 689 | 现货 | ||
10 mg | ¥ 1,120 | 现货 | ||
25 mg | ¥ 2,080 | 现货 | ||
50 mg | ¥ 3,380 | 现货 | ||
100 mg | ¥ 4,820 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 773 | 现货 |
产品描述 | OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors. |
靶点活性 | FLK1:8 nM, CSF1R:15 nM, KDR:9 nM, C-Raf:41 nM, Lck:22 nM |
体外活性 | 在HMC-1, NCI-SNU-5, COLO-205和U251移植瘤模型中,口服OSI-930(200 mg/kg)能够够抑制肿瘤细胞增殖. |
体内活性 | 在HMC-1 细胞系中(IC50=14 nM),OSI-930抑制细胞增殖,诱导细胞凋亡。OSI-930能够抑制多种重组受体酪氨酸激酶,Kit(IC50=80 nM), KDR(IC50=9 nM), Flt( IC50=8 nM), CSF-1R(IC50=15 nM), c-Raf (IC50=41 nM)和Lck(IC50=22 nM)。 |
激酶实验 | Protein kinase assays : Protein kinase assays are either done in-house by ELISA-based assay methods (Kit, KDR, PDGFRα, and PDGFRβ) or by a radiometric method. In-house ELISA assays used poly(Glu:Tyr) as the substrate bound to the surface of 96-well assay plates; phosphorylation is then detected using an antiphosphotyrosine antibody conjugated to HRP. The bound antibody is then quantitated using ABTS as the peroxidase substrate by measuring the absorbance at 405/490 nm. All assays uses purified recombinant kinase catalytic domains that are either expressed in insect cells or in bacteria. The Kit and EGFR protein used for in-house assays are prepared internally; other enzymes are obtained. Recombinant Kit protein is expressed as an NH2-terminal glutathione S-transferase fusion protein in insect cells and is initially purified as a nonphosphorylated (nonactivated) enzyme with a relatively high Km for ATP (400 μM). In some assays, an activated (tyrosine phosphorylated) form of the enzyme is prepared by incubation with 1 mM ATP for 1 hour at 30 °C. The phosphorylated protein is then passed through a desalting column to remove the majority of the ATP and stored at ?80 °C in buffer containing 50% glycerol. The resultant preparation has a considerably higher specific activity and a lower Km for ATP (25 μM) than the initial nonphosphorylated preparation. The inhibition of Kit autophosphorylation by OSI-930 is assayed by incubation of the nonphosphorylated enzyme at 30 °C in the presence of 200 μM ATP and various concentrations of OSI-930. The reaction is stopped by removal of aliquots into SDS-PAGE sample buffer followed by heating to 100 °C for 5 minutes. The degree of phosphorylation of Kit is then determined by immunoblotting for both total Kit and phosphorylated Kit. |
细胞实验 | For assays of cell proliferation and apoptosis, cells are seeded into 96-well plates and incubated for 2 to 3 days in the presence of OSI-930 at various concentrations. Inhibition of cell growth is determined by luminescent quantitation of the intracellular ATP content using CellTiterGlo. Induction of caspase-dependent apoptosis by OSI-930 is quantitated by an enzymatic caspase 3/7 assay. Inhibition of angiogenesis by OSI-930 is monitored using the rat aortic ring endothelial sprout outgrowth assay. Sections of aorta are prepared from CO2-euthanized male rats and cultured in vitro in a collagen matrix in the presence or absence of OSI-930. The collagen matrix is prepared from type 1 rat tail collagen solubilized in 0.1% acetic acid at 3 mg/mL, which is combined with 0.125 volume collagen buffer (0.05 N NaOH, 200 mM HEPES, 260 mM NaHCO3), 0.125 volume of medium 199, 0.0125 volume of 1 M NaOH, and 1% GlutaMax. Aortic rings are embedded in 0.4 mL of this matrix in six-well plates, to which 0.5 mL endothelial basal medium and the appropriate amount of OSI-930 is added; the rings are then incubated for 10 days and the resultant angiogenic sprout outgrowth is digitally quantitated from images by measurement of the sprout-containing area within a series of concentric rings around the aortic tissue area.(Only for Reference) |
别名 | OSI 930, 噻尔非尼 |
分子量 | 443.44 |
分子式 | C22H16F3N3O2S |
CAS No. | 728033-96-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 82 mg/mL (184.9 mM)
Ethanol: 3 mg/mL (6.76 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.2551 mL | 11.2755 mL | 22.551 mL | 56.3774 mL |
5 mM | 0.451 mL | 2.2551 mL | 4.5102 mL | 11.2755 mL | |
DMSO | 10 mM | 0.2255 mL | 1.1275 mL | 2.2551 mL | 5.6377 mL |
20 mM | 0.1128 mL | 0.5638 mL | 1.1275 mL | 2.8189 mL | |
50 mM | 0.0451 mL | 0.2255 mL | 0.451 mL | 1.1275 mL | |
100 mM | 0.0226 mL | 0.1128 mL | 0.2255 mL | 0.5638 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
OSI-930 728033-96-3 Angiogenesis Apoptosis MAPK Tyrosine Kinase/Adaptors c-Kit Src VEGFR c-Fms Raf CSF-1R FLT Inhibitor CD117 Vascular endothelial growth factor receptor CSF1R colony stimulating factor 1 receptor antitumor OSI 930 SCFR selective OSI930 CSF-1 receptor 噻尔非尼 inhibit inhibitor