2. Protein Tyrosine Kinase/RTK Autophagy
  3. VEGFR Autophagy PDGFR
  4. Cediranib

Cediranib  (Synonyms: セジラニブ; AZD2171)

製品番号: HY-10205 純度: 99.87%
COA 取扱説明書 Technical Support

Cediranib (AZD2171) is a highly potent, orally available and blood-brain barrier permeability VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.

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Cediranib

Cediranib 構造式

CAS 番号 : 288383-20-0

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 79 在庫あり
Solution
10 mM * 1 mL in DMSO USD 79 在庫あり
Solid
5 mg $72 在庫あり
10 mg $108 在庫あり
25 mg $170 在庫あり
50 mg $228 在庫あり
100 mg $324 在庫あり
200 mg $588 在庫あり
500 mg   お問い合わせ  
1 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 11 publication(s) in Google Scholar

Other Forms of Cediranib:

Cediranib 関連抗体

Top Publications Citing Use of Products

VEGFR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

PDGFR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PDGFR PDGFRβ PDGFRα

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製品説明

Cediranib (AZD2171) is a highly potent, orally available and blood-brain barrier permeability VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.

IC50 & Target[1]

Flt-1

5 nM (IC50)

KDR

1 nM (IC50)

Flt-4

3 nM (IC50)

PDGFRα

36 nM (IC50)

PDGFRβ

5 nM (IC50)

c-Kit

2 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
BaF3 IC50
1.71 nM
Compound: Cediranib
Antiproliferative activity against VEGFR2-transformed mouse BaF3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
Antiproliferative activity against VEGFR2-transformed mouse BaF3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
[PMID: 37429211]
HCT-116 IC50
1.91 μM
Compound: Cediranib
Antitumor activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
Antitumor activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
[PMID: 37429211]
HeLa IC50
7.67 μM
Compound: Cediranib
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
[PMID: 29624387]
HT-29 IC50
3.45 μM
Compound: Cediranib
Antitumor activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
Antitumor activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
[PMID: 37429211]
HUVEC ED50
0.012 μM
Compound: 5, ZD-2171
Inhibition of VEGF-stimulated HUVEC cell proliferation treated before 2 hrs of VEGF challenge assessed after 3 days by [3H]thymidine incorporation assay
Inhibition of VEGF-stimulated HUVEC cell proliferation treated before 2 hrs of VEGF challenge assessed after 3 days by [3H]thymidine incorporation assay
[PMID: 19101155]
HUVEC IC50
1.2 nM
Compound: Cediranib
Antiproliferative activity against HUVEC assessed as inhibition of human recombinant VEGF165-induced proliferation preincubated for 2 hrs followed by VEGF165 addition measured after 48 hrs by cell counting analysis
Antiproliferative activity against HUVEC assessed as inhibition of human recombinant VEGF165-induced proliferation preincubated for 2 hrs followed by VEGF165 addition measured after 48 hrs by cell counting analysis
10.1039/C5MD00191A
HUVEC IC50
2.14 nM
Compound: Cediranib
Antiproliferative activity against VEGF-stimulated HUVEC assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
Antiproliferative activity against VEGF-stimulated HUVEC assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
[PMID: 37429211]
MDA-MB-231 IC50
3.82 μM
Compound: Cediranib
Antitumor activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
Antitumor activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
[PMID: 37429211]
MDA-MB-468 IC50
3.91 μM
Compound: Cediranib
Antitumor activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
Antitumor activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
[PMID: 37429211]
OVCAR-3 IC50
5.87 μM
Compound: Cediranib
Antitumor activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
Antitumor activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
[PMID: 37429211]
SK-OV-3 IC50
6.68 μM
Compound: Cediranib
Antitumor activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
Antitumor activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay
[PMID: 37429211]
体外実験

In human umbilical vein endothelial cells, Cediranib inhibits VEGF-stimulated proliferation and KDR phosphorylation with IC50 values of 0.4 and 0.5 nM, respectively. In a fibroblast/endothelial cell coculture model of vessel sprouting, Cediranib also reduces vessel area, length, and branching at subnanomolar concentrations[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cediranib 関連抗体
体内実験

Once-daily oral administration of Cediranib ablates experimental (VEGF-induced) angiogenesis and inhibits endochondral ossification in bone or corpora luteal development in ovary; physiologic processes that are highly dependent upon neovascularization. The growth of established human tumor xenografts (colon, lung, prostate, breast, and ovary) in athymic mice is inhibited dose-dependently by Cediranib, with chronic administration of 1.5 mg per kg per day producing statistically significant inhibition in all models. A histologic analysis of Calu-6 lung tumors treated with Cediranib reveals a reduction in microvessel density within 52 hours that becomes progressively greater with the duration of treatment. These changes are indicative of vascular regression within tumors[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

450.51

分子式

C25H27FN4O3
CAS 番号
Appearance

Solid

Color

White to yellow

SMILES

FC1=C(OC2=C(C(C=C3OCCCN4CCCC4)=NC=N2)C=C3OC)C=CC5=C1C=C(C)N5
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 20 mg/mL (44.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2197 mL 11.0985 mL 22.1971 mL
5 mM 0.4439 mL 2.2197 mL 4.4394 mL
10 mM 0.2220 mL 1.1099 mL 2.2197 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2 mg/mL (4.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2 mg/mL (4.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.87%

COA (247 KB) HNMR (253 KB) LCMS (96 KB)

取扱説明書 (2659 KB)
参考文献
キナーゼ実験
[1]

The inhibitory activity of Cediranib is determined against a range of recombinant tyrosine kinases [KDR, Flt-1, Flt-4, c-Kit, PDGFR-α, PDGFR-β, CSF-1R, Flt-3, FGFR1, Src, Abl, epidermal growth factor receptor (EGFR), ErbB2, Aur-A, and Aur-B] using ELISA methodology[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
細胞実験
[1]

Proliferation of MG63 osteosarcoma cells is induced by PDGF-AA, which selectively activates PDGFR-α homodimer signaling. 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 reincubated for 72 hours. Cellular proliferation is determined using a bromodeoxyuridine[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
動物実験
[1]

Rats: Young female Alderley Park rats (6 weeks of age, Wistar derived, n=5) are dosed orally, once daily for 28 days with Cediranib (1.25-5 mg per kg per day) or vehicle. Additional rats (five per group) are treated with Cediranib (5 mg per kg per day) or vehicle for 28 days and maintained for a further 28 days without treatment, to examine the effect of compound withdrawal. Histologic paraffin wax sections of the femorotibial joints and ovaries are stained with H&E. Morphometric image analysis of femorotibial sections is done, with growth plate areas from both the femur and tibia in each joint being combined for an analysis of the effect of compound treatment. The area of corpora lutea in H&E-stained ovary sections is similarly determined by morphometric analysis[1].

Mice: Mice bearing established Calu-6 human lung tumor xenografts (0.2±0.01 cm3) are selected (day 0) and treated chronically with Cediranib (6 mg per kg per day, p.o.) or vehicle. Tumors are collected (6-15 per group) 4 hours after the last dose of Cediranib or vehicle, on days 1, 2, 7, 14, and 21. CD31 is then detected in sections using a chromagen end point or fluorescent immunostaining[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 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 0.2220 mL 1.1099 mL 2.2197 mL 5.5493 mL
15 mM 0.1480 mL 0.7399 mL 1.4798 mL 3.6995 mL
20 mM 0.1110 mL 0.5549 mL 1.1099 mL 2.7746 mL
25 mM 0.0888 mL 0.4439 mL 0.8879 mL 2.2197 mL
30 mM 0.0740 mL 0.3700 mL 0.7399 mL 1.8498 mL
40 mM 0.0555 mL 0.2775 mL 0.5549 mL 1.3873 mL
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Cediranib Related Classifications

  • Molarity Calculator

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cediranib288383-20-0AZD2171AZD 2171AZD-2171VEGFRAutophagyPDGFRVascular endothelial growth factor receptorPlatelet-derived growth factor receptorInhibitorinhibitorinhibit

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