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SU5402

SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.

SU5402化学構造

CAS No. 215543-92-3

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 67000 国内在庫あり
JPY 145500 国内在庫なし(納期7~10日)
JPY 415500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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製品安全説明書

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SU5402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

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
NIH 3T3 Function assay 5 mins Inhibition of FGF induced FGFR1 autophosphorylation in mouse NIH 3T3 cells preincubated for 5 mins followed by FGF-stimulation for 5 mins in presence of [gamma-32P]ATP by SDS-PAGE based autoradiography, IC50=10μM 27914362
HUVEC or NIH3T3 Function assay Evaluated for the inhibition of cell proliferation induced by FGF in HUVEC or NIH3T3 cells, IC50=2.8μM 10893303
HUVEC or NIH3T3 Function assay Evaluated for the inhibition of cell proliferation induced by VEGF in HUVEC or NIH3T3 cells, IC50=0.05μM 10893303
NIH/3T3 Function assay Inhibition of acidic FGF-stimulated FGFR1 tyrosine autophosphorylation in mouse NIH/3T3 cells by immunoblotting, IC50=10μM 9139660
HUVEC or NIH3T3 Function assay Evaluated for the inhibition of cell proliferation induced by PDGF in HUVEC or NIH3T3 cells, IC50=28.4μM 10893303
NIH/3T3 Growth inhibition assay Growth inhibition of mouse NIH/3T3 cells assessed as inhibition of acidic FGF-stimulated [3H]thymidine incorporation 9139660
NIH/3T3 Function assay Inhibition of FGFR1 in mouse NIH/3T3 cells assessed as inhibition of aFGF-stimulated pp90 phosphoprotein phosphorylation by immunoblotting 9139660
NIH/3T3 Function assay Inhibition of FGFR1 in mouse NIH/3T3 cells assessed as inhibition of acidic FGF-stimulated ERK1 phosphorylation by immunoblotting 9139660
NIH/3T3 Function assay Inhibition of FGFR1 in mouse NIH/3T3 cells assessed as inhibition of acidic FGF-stimulated ERK2 phosphorylation by immunoblotting 9139660
NIHIR Function assay Inhibition of insulin-stimulated insulin receptor beta subunit autophosphorylation in mouse NIHIR cells 9139660
HER14 Function assay Inhibition of EGF-stimulated EGFR phosphorylation in mouse HER14 cells by immunoblotting 9139660
HER14 Function assay Inhibition of EGFR in mouse HER14 cells assessed as inhibition of EGF-stimulated Shc phosphorylation by immunoblotting 9139660
HER14 Function assay Inhibition of EGFR in mouse HER14 cells assessed as inhibition of EGF-stimulated ERK2 activation by immunoblotting 9139660
NIHIR Function assay Inhibition of insulin receptor in mouse NIHIR cells assessed as inhibition of insulin-stimulated IRS1 phosphorylation 9139660
NIH/3T3 Function assay Inhibition of PDGFR in mouse NIH/3T3 cells assessed as inhibition of PDGF-stimulated tyrosine autophosphorylation by immunoblotting 9139660
NIH/3T3 Function assay Inhibition of PDGFR in mouse NIH/3T3 cells assessed as inhibition of PDGF-stimulated phospholipase C gamma phosphorylation by immunoblotting 9139660
NIH/3T3 Function assay Inhibition of PDGFR in mouse NIH/3T3 cells assessed as PDGF-stimulated Erk2 activation by immunoblotting 9139660
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生物活性

製品説明 SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.
Targets
VEGFR2 [1]
(Cell-free assay)		 FGFR1 [1]
(Cell-free assay)		 PDGFRβ [1]
(Cell-free assay)
20 nM 30 nM 510 nM
In Vitro
In vitro SU5402 inhibits VEGF-, FGF-, PDGF- dependent cell proliferation with IC50 of 0.05 μM, 2.80μM, 28.4 μM, respectively. [1] In HUVECs, SU5416 selectively inhibits VEGF-driven mitogenesis in a dose-dependent manner with IC50 of 0.04 μM. [2] In nasopharyngeal epithelial cells, SU5402 attenuates LMP1-mediated aerobic glycolysis, cellular transformation, cell migration, and invasion. [3] In mouse C3H10T1/2 cells, SU 5402 diminishes the effect of FGF23 on cell differentiation. [4]
Kinase Assay FGF-R1 and Flk-1/KDR kinase assays.
The catalytic portion of FGF-R1 and Flk-1/KDR are expressed as GST fusion proteins following infection of Spodoptera frugiperda (sf9) cells with engineered baculoviruses. GST-FGFR1 and GST-Flk1 are purified to homogeneity from infected sf9 cell lysates by glutathione sepharose chromatography. The assays are performed in 96-well microtiter plates that had been coated overnight with 2.0 μg of a polyGlu-Tyr peptide (4:1) in 0.1 mL of PBS per well. The purified kinases are diluted in kinase assay buffer (100 mM Hepes pH 7.5, 100 mM NaCl, and 0.1 mM sodium orthovanadate) and added to all test wells at 5 ng of GST fusion protein per 0.05 mL volume buffer. Test compounds are diluted in 4% DMSO and added to test wells (0.025 mL/well). The kinase reaction is initiated by the addition of 0.025 mL of 40 μM ATP/40 mM MnCl2, and plates are shaken for 10 min before stopping the reactions with the addition of 0.025 mL of 0.5 M EDTA. The final ATP concentration was 10 μM, which is twice the experimentally determined Km value for ATP. Negative control wells receive MnCl2 alone without ATP. The plates are washed three times with 10 mM Tris pH 7.4, 150 mM NaCl, and 0.05% Tween-20 (TBST). Rabbit polyclonal anti-phosphotyrosine antiserum is added to the wells at a 1:10000 dilution in TBST for 1 h. The plates are then washed three times with TBST. Goat anti-rabbit antiserum conjugated with horseradish peroxidase was then added to all wells for 1 h. The plates are washed three times with TBST, and the peroxidase reaction is detected with the addition of 2,2‘-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS). The color readout of the assay is allowed to develop for 20−30 min and read on a Dynatech MR5000 ELISA plate reader using a 410 nM test filter.
細胞実験 細胞株 SF767T, SF763, EPH4-VEGF, C6, A375, A431, LNCAP, Calu-6, 3T3Her2 and 488G2M2 cells
濃度 ~50 μM
反応時間 96 hours
実験の流れ Tumor cell lines used in the in vitro growth are cultured in media at 37°C in 5–10% CO2. SU5416 is serially diluted in media containing DMSO (<0.5%) and added to cultures of tumor cells 1 day after the initiation of culture. Cell growth is measured after 96 h using the sulforhodamine B method. IC50s are calculated by curve fitting using four-parameter analysis.
In Vivo
In Vivo In mice, SU5416 (25 mg/kg, i.p.) inhibits subcutaneous growth of a panel of tumor cell lines by inhibiting the angiogenic process associated with tumor growth. [2]
動物実験 動物モデル Mice bearing SF767T, SF763, EPH4-VEGF, C6, A375, A431, LNCAP, Calu-6, 3T3Her2 or 488G2M2 tumors
投与量 25 mg/kg/d
投与経路 i.p.

化学情報

分子量 296.32 化学式

C17H16N2O3
CAS No. 215543-92-3 SDF Download SU5402 SDFをダウンロードする
Smiles CC1=CNC(=C1CCC(=O)O)C=C2C3=CC=CC=C3NC2=O
保管

In vitro
Batch:

DMSO : 59 mg/mL ( (199.1 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

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。

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