ホームページ Protein Tyrosine Kinase c-Met inhibitor - Apoptosis related activator - Autophagy activator SU11274 For research use only.

SU11274

別名：PKI-SU11274

SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest.

SU11274化学構造

CAS No. 658084-23-2

サイズ 価格(税別) 在庫状況
JPY 22000 国内在庫あり
JPY 37000 国内在庫あり
JPY 85500 国内在庫あり
JPY 598500 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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SU11274関連製品

シグナル伝達経路

c-Met Signaling Pathways

c-Metシグナル伝達経路

c-Met阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
DLD1 cells Function assay 2.5 μM 16 h Inhibition of human MET receptor in DLD1 cells at 2.5 uM after 16 hrs by Western blot 17595299
DLD1 cells Function assay 2.5 μM Inhibition of human p38-alpha phosphorylation in DLD1 cells at 2.5 μM 17595299
human MDCK cells Function assay 24 h Inhibition of Met-mediated scattering in HGF-stimulated human MDCK cells pre-incubated overnight prior to HGF stimulation for 24 hrs measured after 24 to 48 hrs, IC50=0.152 μM 22138308
mouse BAF3 cells Proliferation assay 72 h Antiproliferative activity against mouse BAF3 cells expressing TPR-Met after 72 hrs in absence of IL-3, IC50=0.53 μM 21405128
human SNU5 cells Proliferation assay 72 h Antiproliferative activity against human SNU5 cells after 72 hrs, IC50=0.8 μM 21405128
human MKN45 cells Proliferation assay 72 h Antiproliferative activity against human MKN45 cells after 72 hrs, IC50=1.3 μM 21405128
mouse NIH/3T3 cells Proliferation assay 72 h Antiproliferative activity against mouse NIH/3T3 cells expressing TPR-Met after 72 hrs, IC50=2 μM 21405128
human MCF7 cells Proliferation assay 72 h Antiproliferative activity against human MCF7 cells after 72 hrs, IC50=6.2 μM 21405128
human SNU1 cells Proliferation assay 72 h Antiproliferative activity against human SNU1 cells after 72 hrs, IC50=7 μM 21405128
human NCI-H1993 cells Proliferation assay 72 h Antiproliferative activity against human NCI-H1993 cells after 72 hrs, IC50=7.3 μM 21405128
human MDA-MB-231 cells Proliferation assay 72 h Antiproliferative activity against human MDA-MB-231 cells after 72 hrs 21405128
human NCI-H441 cells Proliferation assay 72 h Antiproliferative activity against human NCI-H441 cells after 72 hrs 21405128
human BxPC3 cells Proliferation assay 72 h Antiproliferative activity against human BxPC3 cells after 72 hrs 21405128
A549 cells Function assay Inhibition of human recombinant c-MET kinase in A549 cells assessed as inhibition of HGF-induced cell growth, IC50=0.01 μM 21812414
human HepG2 cells Function assay Inhibition of Met-mediated tumorigenesis in HGF-stimulated human HepG2 cells assessed as impairment in anchorage-independent growth by soft agar growth assay, IC50=1.561 μM 22138308
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生物活性

製品説明 SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest.
Targets
Met [1]
(Cell-free assay)
0.01 μM
In Vitro
In vitro SU11274 exhibits greater than 50-fold selectivity for Met versus Flk and more than 500 times selectivity versus other tyrosine kinases such as FGFR-1, c-src, PDGFbR, and EGFR. SU11274 inhibits the phosphorylation of key regulators of the PI3K pathway, including AKT, FKHR, or GSK3β. SU11274 treatment inhibits the growth of TPR-MET-transformed BaF3 cells in a dose-dependent manner with IC50 of <3 μM in the absence of interleukin 3, without growth inhibition of BaF3 cells transformed by other oncogenic tyrosine kinases, including BCR-ABL, TEL-JAK2, TEL-ABL, and TEL-PDGFβR. In addition to cell growth, SU11274 treatment significantly inhibits the migration of BaF3. TPR-MET cells by 44.8% and 80% at 1 μM and 5 μM, respectively. SU11274 inhibits HGF-dependent phosphorylation of Met as well as HGF-dependent cell proliferation and motility with an IC50 of 1-1.5 μM. In H69 and H345 cells which have functional Met receptor, SU11274 inhibits the HGF-induced cell growth with IC50 of 3.4 μM and 6.5 μM, respectively. SU11274 induces G1 cell cycle arrest with cells in G1 phase increased from 42.4% to 70.6% at 5 μM, and induces caspase-dependent apoptosis by 24% at 1 μM. [2] SU11274 inhibits cell viability in c-Met-expressing non-small cell lung cancer (NSCLC) cells with IC50 values of 0.8-4.4 μM, and abrogates hepatocyte growth factor-induced phosphorylation of c-Met and its downstream signaling. [3]
Kinase Assay In vitro Met kinase assay
A chimeric protein is constructed containing the cytoplasmic domain of human c-Met fused to Glutathione S-transferase (GST) and expressed in SF9 cells. The c-Met kinase GST-fusion protein is used for an ELISA-based Met biochemical assay using the random copolymer poly(Glu:Tyr) (4:1) immobilized on microtiter plates as a substrate. IC50 value is determined with various concentrations of SU11274 in a buffer containing 5 μM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate. The kinase reaction is performed for 5 minutes at room temperature. The extent of substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies.
細胞実験 細胞株 BaF3.TPR-MET, H69 and H345 cells
濃度 Dissolved in DMSO, final concentrations ~10 μM
反応時間 24, 48, and 72 hours
実験の流れ Cells are exposed to various concentrations of SU11274 in the presence or absence of HGF for 24, 48, and 72 hours. The number of viable cells is determined using the MTT assay or trypan blue exclusion. Cell Cycle and apoptosis are measured by fluorescence-activated cell sorter analysis via propidium iodide staining and Annexin V-positive staining, respectively.
実験結果図 Methods Biomarkers 結果図 PMID
Growth inhibition assay Cell viability 23341789
Western blot p-Met / Met / p-AKT / AKT / p-ERK / ERK PUMA / Bcl-2 / Bax 23341789
Immunofluorescence p-SphK1 27864331

化学情報

分子量 568.09 化学式

C28H30CIN5O4S
CAS No. 658084-23-2 SDF Download SU11274 SDFをダウンロードする
Smiles CC1=C(NC(=C1C(=O)N2CCN(CC2)C)C)C=C3C4=C(C=CC(=C4)S(=O)(=O)N(C)C5=CC(=CC=C5)Cl)NC3=O
保管

In vitro
Batch:

DMSO : 92 mg/mL ( (161.94 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。)

Ethanol : 2 mg/mL

Water : 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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Handling Instructions

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よくある質問（FAQ）

質問1:
What is the solubility of S1080 SU11274 in acetone?

回答
The solubility of S1080 SU11274 in acetone is 7 mg/mL.

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