Art. -Nr.: HY-12014

Copy Link Print Information

SU11274

(Synonyms: PKI-SU11274)

8 Cited Publications

Kundenbewertung

Based on 8 publication(s) in Google Scholar

SU11274 is a selective Met inhibitor with IC₅₀ of 10 nM, but has no effects on PGDFRβ, EGFR or Tie2.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.82%
CAS. Nr.: 658084-23-2
Formel: C₂₈H₃₀ClN₅O₄S
Molecular Weight:568.09

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SU11274 Chemical Structure

CAS. Nr.: 658084-23-2

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SU11274 is a selective Met inhibitor with IC₅₀ of 10 nM, but has no effects on PGDFRβ, EGFR or Tie2.

IC₅₀ & Target

IC50: 10 nM (Met)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	<3 μM Compound: SU11274	Inhibition of cell growth in mouse BaF3 cells transfected with TPR-MET genes by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay Inhibition of cell growth in mouse BaF3 cells transfected with TPR-MET genes by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay	[PMID: 14500382]
BaF3	IC₅₀	0.53 μM Compound: 2, SU11274	Antiproliferative activity against mouse BAF3 cells expressing TPR-Met after 72 hrs in absence of IL-3 Antiproliferative activity against mouse BAF3 cells expressing TPR-Met after 72 hrs in absence of IL-3	[PMID: 21405128]
BaF3	IC₅₀	6.4 μM Compound: 2, SU11274	Antiproliferative activity against mouse BAF3 cells expressing TPR-Met after 72 hrs in presence of IL-3 Antiproliferative activity against mouse BAF3 cells expressing TPR-Met after 72 hrs in presence of IL-3	[PMID: 21405128]
BXPC-3	IC₅₀	16 μM Compound: 2, SU11274	Antiproliferative activity against human BxPC3 cells after 72 hrs Antiproliferative activity against human BxPC3 cells after 72 hrs	[PMID: 21405128]
HepG2	IC₅₀	1.561 μM Compound: SU, SU11274	Inhibition of Met-mediated tumorigenesis in HGF-stimulated human HepG2 cells assessed as impairment in anchorage-independent growth by soft agar growth assay Inhibition of Met-mediated tumorigenesis in HGF-stimulated human HepG2 cells assessed as impairment in anchorage-independent growth by soft agar growth assay	[PMID: 22138308]
MCF7	IC₅₀	6.2 μM Compound: 2, SU11274	Antiproliferative activity against human MCF7 cells after 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs	[PMID: 21405128]
MDA-MB-231	IC₅₀	11 μM Compound: 2, SU11274	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs	[PMID: 21405128]
MDCK	IC₅₀	0.152 μM Compound: SU, SU11274	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 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	[PMID: 22138308]
MDCK	IC₅₀	0.2 μM Compound: SU11274	Inhibition of Met-triggered cell scattering in HGF-stimulated MDCK cells preincubated for overnight before HGF challenge measured after 24 to 48 hrs Inhibition of Met-triggered cell scattering in HGF-stimulated MDCK cells preincubated for overnight before HGF challenge measured after 24 to 48 hrs	[PMID: 22738633]
MKN-45	IC₅₀	1.3 μM Compound: 2, SU11274	Antiproliferative activity against human MKN45 cells after 72 hrs Antiproliferative activity against human MKN45 cells after 72 hrs	[PMID: 21405128]
NCI-H1993	IC₅₀	7.3 μM Compound: 2, SU11274	Antiproliferative activity against human NCI-H1993 cells after 72 hrs Antiproliferative activity against human NCI-H1993 cells after 72 hrs	[PMID: 21405128]
NCI-H441	IC₅₀	13 μM Compound: 2, SU11274	Antiproliferative activity against human NCI-H441 cells after 72 hrs Antiproliferative activity against human NCI-H441 cells after 72 hrs	[PMID: 21405128]
NIH3T3	IC₅₀	≥ 50 μM Compound: 2, SU11274	Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs	[PMID: 21405128]
NIH3T3	IC₅₀	2 μM Compound: 2, SU11274	Antiproliferative activity against mouse NIH/3T3 cells expressing TPR-Met after 72 hrs Antiproliferative activity against mouse NIH/3T3 cells expressing TPR-Met after 72 hrs	[PMID: 21405128]
SNU1	IC₅₀	7 μM Compound: 2, SU11274	Antiproliferative activity against human SNU1 cells after 72 hrs Antiproliferative activity against human SNU1 cells after 72 hrs	[PMID: 21405128]
SNU-5	IC₅₀	0.8 μM Compound: 2, SU11274	Antiproliferative activity against human SNU5 cells after 72 hrs Antiproliferative activity against human SNU5 cells after 72 hrs	[PMID: 21405128]

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].

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

Chemical Information

CAS. Nr. 658084-23-2
Appearance Solid
Molecular Weight 568.09
Formel C₂₈H₃₀ClN₅O₄S
Color White to yellow
SMILES

O=S(C1=CC2=C(C=C1)NC(/C2=C/C3=C(C(C(N4CCN(CC4)C)=O)=C(N3)C)C)=O)(N(C)C5=CC=CC(Cl)=C5)=O
Synonyms

PKI-SU11274
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

All Cell Proliferation/Viability AssayRT-PCRWBIHCCell Imaging/Staining

Sort by:

Journal Impact Factor

Cell Rep

Endocytic activation and exosomal secretion of matriptase stimulate the second wave of EGF signaling to promote skin and breast cancer invasion. [Abstract]

2024 Mar 27;43(4):114002. PMID: 38547126
Cancer Cell Int

Human colorectal cancer-derived carcinoma associated fibroblasts promote CD44-mediated adhesion of colorectal cancer cells to endothelial cells by secretion of HGF. [Abstract]

2019 Jul 24:19:192. PMID: 31367190
Cells

SMYD3 Modulates the HGF/MET Signaling Pathway in Gastric Cancer. [Abstract]

2023 Oct 18;12(20):2481. PMID: 37887325

SU11274 purchased from MedChemExpress. Usage Cited in: Cells. 2023 Oct 18;12(20):2481. [Abstract]

Quantification of cell proliferation by Cell Titer Glo in GC cell lines. Cells were treated with increasing doses of SU11274 (5, 10 μM) for up to 48 h.

SU11274 purchased from MedChemExpress. Usage Cited in: Cells. 2023 Oct 18;12(20):2481. [Abstract]

Immunoblot analysis showing phosphoactivation of MET, ERK 1/2, and AKT in GC cell lines treated with 10 μM SU11274 for 48 h.

SU11274 purchased from MedChemExpress. Usage Cited in: Cells. 2023 Oct 18;12(20):2481. [Abstract]

Live and dead staining of GC tumorspheres grown as 3D cocultures with CAFs and treated with 5 μM EM127 and/or 10 μM SU11274 for 48 h.
Biochim Biophys Acta Mol Cell Res

Hepatocyte growth factor attenuates high glucose-disturbed mitochondrial dynamics in podocytes by decreasing ARF6-dependent DRP1 translocation. [Abstract]

2023 Oct 31;1871(1):119623. PMID: 37913847
Regen Ther

Iron-Quercetin complex enhances mesenchymal stem cell-mediated HGF secretion and c-Met activation to ameliorate acute kidney injury through the prevention of tubular cell apoptosis. [Abstract]

2024 Dec 17:28:169-182. PMID: 39802634

SU11274 purchased from MedChemExpress. Usage Cited in: Regen Ther. 2024 Dec 17:28:169-182. [Abstract]

Effect of su11274 on the mRNA expression of bax, caspase 3 and bcl2 in RT-PCR.

SU11274 purchased from MedChemExpress. Usage Cited in: Regen Ther. 2024 Dec 17:28:169-182. [Abstract]

The results of H&E, PAS and IHC (Kim 1) staining treated with su11274 (0.2 mg/kg, i.p.).
Pediatr Surg Int

Epidermal growth factor receptor/heme oxygenase-1 axis is involved in chemoresistance to cisplatin and pirarubicin in HepG2 cell lines and hepatoblastoma specimens. [Abstract]

2019 Dec;35(12):1369-1378. PMID: 31559456
University of South Dakota

2026.
bioRxiv

Ras-Responsive Element Binding Protein 1 regulates survival of Group 3 medulloblastoma. [Abstract]

2025 Jul 21:2025.07.16.665230. PMID: 40777316

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (176.03 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7603 mL

8.8014 mL

17.6028 mL

5 mM

0.3521 mL

1.7603 mL

3.5206 mL

10 mM

0.1760 mL

0.8801 mL

1.7603 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.5 mg/mL (4.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

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.

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

Cell Assay^[2]

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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wang X, et al. Potent and selective inhibitors of the Met [hepatocyte growth factor/scatter factor (HGF/SF) receptor] tyrosine kinase block HGF/SF-induced tumor cell growth and invasion. Mol Cancer Ther, 2003, 2(11):1085-1092. [Content Brief]

[2]. Sattler M, et al. A novel small molecule met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase. Cancer Res, 2003, 63(17), 5462-5469. [Content Brief]

[3]. Ma PC, et al. Functional expression and mutations of c-Met and its therapeutic inhibition with SU11274 and small interfering RNA in non-small cell lung cancer. Cancer Res, 2005, 65(4), 1479-1488. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7603 mL	8.8014 mL	17.6028 mL	44.0071 mL
	5 mM	0.3521 mL	1.7603 mL	3.5206 mL	8.8014 mL
	10 mM	0.1760 mL	0.8801 mL	1.7603 mL	4.4007 mL
	15 mM	0.1174 mL	0.5868 mL	1.1735 mL	2.9338 mL
	20 mM	0.0880 mL	0.4401 mL	0.8801 mL	2.2004 mL
	25 mM	0.0704 mL	0.3521 mL	0.7041 mL	1.7603 mL
	30 mM	0.0587 mL	0.2934 mL	0.5868 mL	1.4669 mL
	40 mM	0.0440 mL	0.2200 mL	0.4401 mL	1.1002 mL
	50 mM	0.0352 mL	0.1760 mL	0.3521 mL	0.8801 mL
	60 mM	0.0293 mL	0.1467 mL	0.2934 mL	0.7335 mL
	80 mM	0.0220 mL	0.1100 mL	0.2200 mL	0.5501 mL
	100 mM	0.0176 mL	0.0880 mL	0.1760 mL	0.4401 mL

Keywords

SU11274

8 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

SU11274

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Peptidomimetic Library

Covalent Screening Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SU11274

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SU11274

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Peptidomimetic Library

Covalent Screening Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SU11274

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SU11274 Related Classifications

HY-12014 Related Classifications