Cediranib (AZD2171)

製品コードS1017 別名:NSC-732208

Cediranib (AZD2171)化学構造

分子量(MW):450.51

Cediranib (AZD2171)は一種の高度有効なVEGFR(KDR)阻害剤で、IC50値が1 nM以下です。同時に、Cediranib (AZD2171)はFlt1/4も抑制して、IC50値が5 nM/3 nM以下に分かれます。尚、Cediranib (AZD2171)はc-KitとPDGFRβにも類似の抑制活性をしています。Cediranib (AZD2171)は、VEGFRに作用する選択性はPDGFR-α、CSF-1RとFlt3に作用する選択性より36倍、110倍と1000倍以上がそれぞれ高くなります。臨床3期。

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カスタマーフィードバック(5)

  • Western blots of EZH2 expression in A549, HCC461, and HCC4006 cells upon treatment with different doses of VEGFR-2-inhibitor AZD2171 (0, 5 and 10 nM). AZD2171 decreased the expression of EZH2 in HCC4006 and HCC461 cells expressing VEGFR-2 in a dose-dependent manner but did not do so in A549 cells lacking expression of VEGFR-2.

    Clin Cancer Res 2014 20, 3849-61. Cediranib (AZD2171) purchased from Selleck.

    Representative histological tumor sections with CD31 vascular staining (brown) and hematoxylin nuclear counterstain (blue) from the 4 treatment groups(untreated, quinacrine, cediranib, ced+quin). Discrete staining is associated with vascular endothelial cells, whereas more diffuse and variable staining is nonspecific and associated with tumor necrosis. Microvessel examples are marked by arrows.

    Neuro Oncol 2013 15, 1673-83. Cediranib (AZD2171) purchased from Selleck.

  • (A) Representative LC3 Western blots obtained from 4C8 cells grown under normoxic (20% O2) or hypoxic (0.5% O2) conditions for 10 h while untreated or exposed to cediranib (3 uM), quinacrine (0.8 uM), or combined cediranib/quinacrine. (B) RFP-LC3-expressing 4C8 cells were visualized using EVOS fl microscopy, grown under hypoxic conditions for 24 h while untreated or exposed to cediranib (2.5 uM), quinacrine (2.5 uM), or combined cediranib/quinacrine. (C) Representative cleaved caspase-3 Western blots obtained from 4C8 cells grown under normoxic (20% O2) or hypoxic (0.5% O2) conditions for 72 h while untreated or exposed to cediranib (2 uM), quinacrine (2 uM), or combined cediranib/quinacrine.

    Neuro Oncol 2013 15, 1673-83. Cediranib (AZD2171) purchased from Selleck.

    Inhibition of P-gp and Bcrp by cediranib. Accumulation of [3H]vin-blastine in MDR1-transfected cells and [3H]prazosin in Bcrp1-transfected cells in the presence of increasing concentrations of cediranib ranging from 0 to 40 μM is shown. 

    J Pharmacol Exp Ther 2012 341, 386-395 . Cediranib (AZD2171) purchased from Selleck.

  • Ba/F3 cell lines expressing the recombinant TEL/kinase domain fusion protein for FGFR1-4 .Cells were grown in RPMI 1640 containing 10% FBS and 500 ng/mL puromycin. The parental Ba/F3 cell line transduced with an empty vector was grown in 10 ng/mL IL-3 (R & D systems). Cell viability was assessed at 72 hours using the Cell Titer 96 Aqueous One Solution (Promega). Data were plotted as percent viability relative to vehicle-treated cells and are shown as mean (±SD) from 3 experiments.

     

     

    Dr. Mikhail Menshikov of Cardiology Research Center. Cediranib (AZD2171) purchased from Selleck.

製品安全説明書

VEGFR阻害剤の選択性比較

生物活性

製品説明 Cediranib (AZD2171)は一種の高度有効なVEGFR(KDR)阻害剤で、IC50値が1 nM以下です。同時に、Cediranib (AZD2171)はFlt1/4も抑制して、IC50値が5 nM/3 nM以下に分かれます。尚、Cediranib (AZD2171)はc-KitとPDGFRβにも類似の抑制活性をしています。Cediranib (AZD2171)は、VEGFRに作用する選択性はPDGFR-α、CSF-1RとFlt3に作用する選択性より36倍、110倍と1000倍以上がそれぞれ高くなります。臨床3期。
ターゲット
VEGFR2/KDR [1]
(HUVECs)
c-Kit [1]
(HUVECs)
VEGFR3/FLT4 [1]
(HUVECs)
VEGFR1/FLT1 [1]
(HUVECs)
PDGFRβ [1]
(HUVECs)
0.5 nM 2 nM <=3 nM 5 nM 5 nM
体外試験

Cediranib inhibits VEGF-stimulated proliferation with IC50 of 0.4 nM. Cediranib suppresses PDGF-AA with IC50 of 0.04 μM in MG63 cell lines. Cediranib has been shown to block Flt1-associated kinase with IC50 of 5 nM and VEGF-C and VEGF-D receptor Flt-4 with IC50 less than 3 nM. In addition, the IC50 values for inhibition of c-Kit and PDGFRβ tyrosine kinase are 2 nM and 5 nM respectively. Furthermore, no inhibition of enzyme activity is observed when 10 μM Cediranib is assayed with 100 μM ATP against AMPK, Chk1 Akt/PKB and others. Micromolar concentrations of Cediranib are needed to prevent tumor cell proliferation in vitro. [1]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HUVEC cell MmLBVJJwdGmoZYLheIlwdiCjc4PhfS=> MX[zJIRigXN? M3Hjb2lvcGmkaYTpc44hd2ZiVlXHSk1{fGmvdXzheIVlKEiXVlXDJINmdGxicILvcIln\XKjdHnvckB1emWjdHXkJIJm\m:{ZTCyJIhzeyCxZjDWSWdHKGOqYXzs[Y5o\SCjc4Pld5Nm\CCjZoTldkA{KGSjeYOgZpkhYzOKXYTofY1q\GmwZTDpcoNwenCxcnH0bY9vKGG|c3H5MEBGTDVyPUGyJI5O Mnq1NVkyODFzNUW=

多くの細胞株試験データを見る場合、クリックしてください

体内試験 Cediranib even suppresses tubule sprouting at subnanomolar concentrations and inhibits VEGF-induced angiogenesis. Cediranib causes hypertrophy in bone growth plate and prevents luteal development in ovary. These are physiological processes that are dependent upon angiogenesis. Cediranib shows broad spectrum activity in human tumor models at doses that are well tolerated. [1] Besides, Cediranib causes regression of vascular tissues in human lung tumor xenografts. [2]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

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.
細胞試験: [1]
+ 展開
  • 細胞株: HUVEC cell line
  • 濃度: 10 μM
  • 反応時間: 72 hours
  • 実験の流れ: 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.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: PC-3, Calu-6, SKOV-3, MDA-MB-231, and SW620 tumors in female nude (nu/nu genotype) mice
  • 製剤: Suspended in 1% (w/v) aqueous polysorbate 80
  • 投薬量: 0.75-6 mg/kg/day
  • 投与方法: Orally
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 90 mg/mL (199.77 mM)
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
5% DMSO+50% PEG 300+5% Tween+ddH2O
5mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 450.51
化学式

C25H27FN4O3

CAS No. 288383-20-0
保管
in solvent
別名 NSC-732208

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02484404 Recruiting Lung Cancer|Breast Cancer|Ovarian Cancer|Colorectal Cancer|Prostate Cancer|Triple Negative Breast Cancer National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) June 4, 2015 Phase 1|Phase 2
NCT02974621 Not yet recruiting Recurrent Glioblastoma National Cancer Institute (NCI) September 2017 Phase 2
NCT02889900 Recruiting Recurrent Platinum Resistant Ovarian Cancer AstraZeneca|Myriad Genetic Laboratories, Inc. January 2017 Phase 2
NCT02893917 Suspended Hormone-Resistant Prostate Cancer|Metastatic Prostate Carcinoma|Prostate Adenocarcinoma With Focal Neuroendocrine Differentiation|Prostate Carcinoma Metastatic in the Bone|Prostate Small Cell Carcinoma|Stage IV Prostate Adenocarcinoma National Cancer Institute (NCI) December 2016 Phase 2
NCT02899728 Not yet recruiting Small Cell Lung Carcinoma National Cancer Institute (NCI) November 2016 Phase 2
NCT02855697 Not yet recruiting Ovarian Cancer Anna Thomason|The Christie NHS Foundation Trust November 2016 Early Phase 1

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

VEGFR信号経路図

VEGFR Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID