Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Orantinib (NSC 702827) 是一种多靶点受体酪氨酸激酶抑制剂,对 Flt-1、PDGFRβ和FGFR1的Ki 值分别为 2.1 μM、8 nM 和 1.2 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 258 | 现货 | ||
5 mg | ¥ 413 | 现货 | ||
10 mg | ¥ 622 | 现货 | ||
25 mg | ¥ 1,150 | 现货 | ||
50 mg | ¥ 1,970 | 现货 | ||
100 mg | ¥ 3,230 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 455 | 现货 |
产品描述 | Orantinib (NSC 702827) , a excellent effective against PDGFR autophosphorylation with Ki of 8 nM, also highly inhibits Flk-1 and FGFR1 trans-phosphorylation. It shows little effect against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2 and does not suppresses EGFR. |
靶点活性 | PDGFRβ:8 nM(Ki) |
体外活性 | 在HT29人类结肠癌肿瘤模型中,TSU-68(200 mg/kg)降低肿瘤边缘的平均血管通透性和肿瘤中心的平均血浆容积分数.在携带多种移植瘤的无胸腺小鼠,包括A375,Colo205,H460,Calu-6,C6,SF763T,和SKOV3TP5细胞等,TSU-68(75-200 mg/kg)抑制细胞生长.兔VX2肝脏肿瘤模型中, TSU-68(200 mg/kg)增加注射化学治疗的效果.在C6神经胶细胞移植瘤中, TSU-68(75 mg/kg)也阻断肿瘤血管生成. |
体内活性 | TSU-68是ATP竞争性抑制剂, 作用于Flk-1/KDR磷酸转移, FGFR1磷酸转移,和PDGFRβ激酶时, Ki分别为2.1 μM, 1.2 μM,和8 nM。在人类骨髓性白血病MO7E细胞中,TSU-68(IC50=0.1-1 μM)抑制肝细胞因子受体c-kit的酪氨酸自磷酸化, 也抑制ERK1/2磷酸化。在SCF刺激的MO7E细胞中,TSU-68(IC50=0.29 μM)也抑制细胞增殖,并诱导凋亡。过量表达PDGFRβ的NIH-3T3细胞中,TSU-68(0.03-0.1 μM)抑制PDGF刺激的PDGFRβ 酪氨酸磷酸化。在血管内皮生长因子刺激的HUVECs中,TSU-68(0.03-10 μM)抑制KDR酪氨酸磷酸化。在过量表达EGFR 的NIH-3T3细胞中, TSU-68(100 μM) 不抑制EGF刺激的EGFR酪氨酸磷酸化。TSU-68抑制血管内皮生长因子驱动的和FGF驱动的HUVECs分裂,平均IC50分别为0.34和 9.6 μM。 |
激酶实验 | trans-Phosphorylation Reactions: Tyrosine kinase assays to quantitate the trans-phosphorylation activity of Flk-1 and FGFR1 are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with 1-5% (w/v) BSA in PBS. Purified GST-FGFR1 (kinase domain) or GST-Flk-1 (cytoplasmic domain) fusion proteins are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-Flk-1 and GST-FGFR1 is 50 ng/mL. SU6668 is dissolved in DMSO at 100× the final required concentration and diluted 1:25 in Water. Twenty-five μL of diluted SU6668 are subsequently added to each reaction well. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 min at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1: 10000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat anti-rabbit antisera conjugated with HRP. The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2 |
细胞实验 | Cells are seeded (3 × 105 cells/35-mm well) in DMEM containing 10% (v/v) FBS and grow to confluence and then quiesced in DMEM containing 0.1% serum for 2 hours before drug treatment. HUVECs (seeded at 2 × 106 cells/10-cm plate) are grown to confluence in endothelial cell growth media and then quiesced in endothelial cell basal media containing 0.5% FBS for 24 hours before drug treatment. All cell lines are incubated with SU6668 for 1 hour before ligand stimulation (100 ng/mL) for 10 min. Western blotting is perfor (Only for Reference) |
别名 | SU6668, TSU-68, NSC 702827 |
分子量 | 310.35 |
分子式 | C18H18N2O3 |
CAS No. | 252916-29-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
1eq. NaOH: 31 mg/mL (100 mM)
DMSO: 31 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
1eq. NaOH / DMSO | 1 mM | 3.2222 mL | 16.1108 mL | 32.2217 mL | 80.5542 mL |
5 mM | 0.6444 mL | 3.2222 mL | 6.4443 mL | 16.1108 mL | |
10 mM | 0.3222 mL | 1.6111 mL | 3.2222 mL | 8.0554 mL | |
20 mM | 0.1611 mL | 0.8055 mL | 1.6111 mL | 4.0277 mL | |
50 mM | 0.0644 mL | 0.3222 mL | 0.6444 mL | 1.6111 mL | |
100 mM | 0.0322 mL | 0.1611 mL | 0.3222 mL | 0.8055 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。
Orantinib 252916-29-3 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors VEGFR FGFR PDGFR inhibit TSU68 Platelet-derived growth factor receptor NSC-702827 SU6668 TSU 68 TSU-68 Vascular endothelial growth factor receptor Inhibitor SU-6668 NSC 702827 NSC702827 SU 6668 Fibroblast growth factor receptor inhibitor