ホームページ Protein Tyrosine Kinase VEGFR inhibitor - c-Kit inhibitor - PDGFR inhibitor Axitinib For research use only.

Axitinib

別名：AG 013736

Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.

Axitinib化学構造

CAS No. 319460-85-0

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 37000 国内在庫あり
JPY 118500 国内在庫あり

代表番号: 045-509-1970|電子メール：sales@selleck.co.jp
よく尋ねられる質問

製品安全説明書

現在のバッチを見る： 純度： 99.96%
99.96

Axitinib関連製品

シグナル伝達経路

VEGFR Signaling Pathways

VEGFRシグナル伝達経路

VEGFR阻害剤の選択性比較

1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
MCF7 Antiproliferative assay 5 days Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 0.97 μM. 23829549
MDA-MB-468 Antiproliferative assay 5 days Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 1.3 μM. 23829549
HCC1954 Antiproliferative assay 5 days Antiproliferative activity against human HCC1954 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 2.7 μM. 23829549
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明 Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.
特性 Superior as second-line therapy relative to sorafenib (current standard-of-care).
Targets
VEGFR1/FLT1 [1]
(Porcine aorta endothelial cells)		 VEGFR2/Flk1 [1]
(Porcine aorta endothelial cells)		 VEGFR2/KDR [1]
(Porcine aorta endothelial cells)		 VEGFR3 [1]
(Porcine aorta endothelial cells)		 PDGFRβ [1]
(Porcine aorta endothelial cells)		 もっとクリックする
0.1 nM 0.18 nM 0.2 nM 0.1 nM-0.3 nM 1.6 nM
In Vitro
In vitro Axitinib could block the cellular autophosphorylation of VEGFR and VEGF-mediated endothelial cell viability, tube formation, and downstream signaling. Axitinib inhibits the proliferation of variable cell lines with IC50 of >10,000 nM (IGR-N91), 849 nM (IGR-NB8), 274 nM (SH-SY5Y) and 573 nM (non-VEGF stimulated HUVEC). [2]
Kinase Assay Cellular receptor kinase phosphorylation assay
Porcine aorta endothelial (PAE) cells, which overexpress full-length VEGFR2, PDGFRβ, Kit, and NIH-3T3, which overexpress murine VEGFR2 (Flk-1) or PDGFRα, are generated. The 96-well plates are coated with 100 μL/well of 2.5 μg/mL anti-VEGFR2 antibody, 0.75 μg/mL anti-PDGFRβ antibody, 0.25 μg/mL anti-PDGFRα antibody, 0.5 μg/mL anti-KIT antibody, or 1.20 μg/mL anti-Flk-1 antibody to prepare ELISA capture plates. Then phosphorylation of RTK is measured by ELISA.
細胞実験 細胞株 HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cells
濃度 1 nM - 10 μM
反応時間 72 hours
実験の流れ

Cells are seeded in a 96-well plate at a density of 5 × 104 and cultured for 24 hours. Axitinib is added to the cells at concentrations ranging from 1 nM to 10 μM. Cell viability is measured after 72 hours by MTS tetrazolium substrate and IC50 values are calculated.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-c-kit / c-kit / p-AKT / AKT / p-ERK / ERK / p-STAT3 / STAT3 / p-STAT5 / STAT5 / p-S6K / S6K / p-S6 / S6 PARP / cleaved PARP / caspase-3 / cleaved caspase-3 31205508
Immunofluorescence alpha-tubulin 26474283
Growth inhibition assay Cell viability 26474283
In Vivo
In Vivo Axitinib exhibits primary inhibition to orthotopically transplanted models such as M24met (melanoma), HCT-116 (colorectal cancer), and SN12C (renal cell carcinoma). [1] Axitinib delays the tumor growth with 11.4 days compared to the controls (p.o. 30 mg/kg) and decreases the Mean Vessels Density (MVD) to 21, compared to 49 in controls, in IGR-N91 flank xenografts. [2] Axitinib significantly inhibits growth and disrupts tumor microvasculature in BT474 breast cancer model at 10-100 mg/kg. [3] Axitinib has shown single-agent activity in variable tumors, including renal cell carcinoma, thyroid cancer, non-small cell lung cancer, and melanoma.
動物実験 動物モデル BT474 breast cancer cells are implanted subcutaneously into Immune-deficient female mice (Nu/nu; age 8-12 weeks).
投与量 10, 30 or 100 mg/kg
投与経路 Oral daily
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06161558 Not yet recruiting
Neoplasms
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 May 15 2024 Phase 1
NCT05949632 Recruiting
Advanced Solid Tumors
Incyte Corporation
 April 16 2024 Phase 1|Phase 2
NCT05969496 Recruiting
Renal Cancer|Kidney Cancer|Renal Cell Carcinoma|Inferior Vena Cava Thrombosis
University of Colorado Denver|Cancer League of Colorado
 December 4 2023 Phase 2
NCT05904730 Enrolling by invitation
Breast Cancer|Ovarian Cancer|Breast Neoplasms|Ovarian Neoplasms|BRCA Mutation|HER2-positive Breast Cancer|HER2-negative Breast Cancer|HER-2 Protein Overexpression
Lynkcell Europe
 July 11 2023 Phase 1
NCT05817903 Recruiting
Metastatic Renal Cell Carcinoma
Consorzio Oncotech|Pfizer
 April 18 2023 Phase 2
NCT05263609 Withdrawn
Renal Cell Cancer
University of Oklahoma|Merck Sharp & Dohme LLC|Pfizer
 June 2022 Phase 2

化学情報

分子量 386.47 化学式

C22H18N4OS
CAS No. 319460-85-0 SDF Download Axitinib SDFをダウンロードする
Smiles CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)C=CC4=CC=CC=N4
保管

In vitro
Batch:

DMSO : 26 mg/mL ( (67.27 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機
Clear solution
5% DMSO 95% Corn oil
0.2mg/ml (0.52mM) Taking the 1 mL working solution as an example, add 50 μL of 4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 40% 5% 50%ddH2O
1.85mg/ml (4.79mM) Taking the 1 mL working solution as an example, add 50 μL of 37 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

大学・企業名を記入してください
名前を記入してください
電子メール・アドレスを記入してください 有効なメールアドレスを入力してください
お問い合わせ内容をご入力ください

よくある質問（FAQ）

質問1:
We would like to store at -80℃ after it dissolved in CMC. Do you have any infomation about the suggested concentration in CMC?

回答
Axitinib in 0.5% CMC at up to 30mg/ml is a suspension for oral gavage administration only. We don't suggest customer to freeze down the solution but to make fresh if possible. Customer can store it for 1-2 weeks at 4 degree for continuous use.

Tags: Axitinibを買う | Axitinib ic50 | Axitinib供給者 | Axitinibを購入する | Axitinib費用 | Axitinib生産者 | オーダーAxitinib | Axitinib化学構造 | Axitinib分子量 | Axitinib代理店