Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Cediranib (AZD2171) 是一种可口服的高选择性VEGFR2抑制剂,对Flt1、KDR、Flt4、PDGFRα、PDGFRβ和c-Kit 的IC50值分别为小于1、小于3、5、5、36和 2nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 269 | 现货 | ||
2 mg | ¥ 378 | 现货 | ||
5 mg | ¥ 589 | 现货 | ||
10 mg | ¥ 897 | 现货 | ||
25 mg | ¥ 1,460 | 现货 | ||
50 mg | ¥ 1,980 | 现货 | ||
100 mg | ¥ 3,320 | 现货 | ||
200 mg | ¥ 4,880 | 现货 | ||
500 mg | ¥ 7,670 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 657 | 现货 |
产品描述 | Cediranib (AZD2171) (AZD2171) is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1/4 (IC50: 5 nM/≤3 nM), similar activity against PDGFRβ and c-Kit, selective more for VEGFR than PDGFR-α (36-fold), CSF-1R (110-fold), and Flt3 (1000-fold) in HUVEC cells. |
靶点活性 | Flt1:5 nM, Flt4:≤3 nM |
体外活性 | Cediranib对人类移植瘤模型具有十分有效的作用且有剂量依赖性.此外,Cediranib可使人肺癌移植瘤血管衰退.Cediranib使骨骼过度生长,对卵巢中黄体的产生具有阻碍作用,并抑制依赖于血管生成的生理程序. |
体内活性 | 在体外,Cediranib(微摩)可直接抑制肿瘤细胞增殖。Cediranib(次纳摩)阻断细管产生,且对体内VEGF诱导的血管生成有抑制作用。Cediranib对bFGF(IC50:0.5 μM)和EGF(IC50:0.11 μM)有抑制作用。在MG63细胞系中,Cediranib抑制PDGF-AA(IC50:0.04 μM)。Cediranib抑制 Flt-1相关激酶(IC50:5 nM),还对VEGF-C和VEGF-D受体Flt-4有抑制作用(IC50<3 nM)。此外,Cediranib对c-Kit(IC50:2 nM)和PDGFR-β(IC50:5 nM)酪氨酸激酶有抑制作用。 |
激酶实验 | Kinase inhibition: Cediranib is dissolved in DMSO at a concentration of 10 mM. All enzyme assays are run at, or just below, the respective Km for ATP (0.2 - 30 μM). The inhibitory activity of Cediranib is determined against a range of recombinant tyrosine kinases [KDR, Flt-1, Flt-4, c-Kit, PDGFRα, PDGFRβ, CSF-1R, Flt-3, FGFR1, Src, Abl, epidermal growth factor receptor (EGFR), ErbB2, Aurora A, and Aurora B] using ELISA. Selectivity versus CDK2 and CDK4 serine/threonine kinases is examined using scintillation proximity assays with a retinoblastoma substrate and [γ-sup>33P]ATP. Activity of Cediranib is compared to MAPK kinase (MEK), which shows dual specificity. It is determined using a MAPK substrate, [γ-33P]ATP, and paper capture/scintillation counting. |
细胞实验 | The proliferation of the HUVEC cell line is evaluated in the presence and absence of growth factors by measuring 3H-thymidine incorporation following a 4-day incubation period. Proliferation of MG63 osteosarcoma cells is induced by PDGF-AA, which selectively activates signaling of the PDGFRα homodimer. HUVEC and MG63 osteosarcoma cells are cultured in DMEM without phenol red containing 1% charcoal stripped FCS, 2 mM glutamine, and 1% nonessential amino acids for 24 hours. Cediranib or vehicle is added with PDGF-AA ligand (50 ng/mL) and plates incubated for another 72 hours. Cellular proliferation is determined using bromodeoxyuridine ELISA. (Only for Reference) |
别名 | AZD2171, NSC-732208, 西地尼布 |
分子量 | 450.51 |
分子式 | C25H27FN4O3 |
CAS No. | 288383-20-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 83 mg/mL (184.2 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2197 mL | 11.0985 mL | 22.1971 mL | 55.4927 mL |
5 mM | 0.4439 mL | 2.2197 mL | 4.4394 mL | 11.0985 mL | |
10 mM | 0.222 mL | 1.1099 mL | 2.2197 mL | 5.5493 mL | |
20 mM | 0.111 mL | 0.5549 mL | 1.1099 mL | 2.7746 mL | |
50 mM | 0.0444 mL | 0.222 mL | 0.4439 mL | 1.1099 mL | |
100 mM | 0.0222 mL | 0.111 mL | 0.222 mL | 0.5549 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。
Cediranib 288383-20-0 Angiogenesis Autophagy Tyrosine Kinase/Adaptors FLT VEGFR PDGFR c-Kit Platelet-derived growth factor receptor Vascular endothelial growth factor receptor inhibit AZD2171 NSC-732208 NSC732208 AZD 2171 NSC 732208 西地尼布 AZD-2171 Inhibitor inhibitor