SU11274 (Synonyms: PKI-SU11274)

Name: SU11274
Brand: MedChemExpress
SKU: HY-12014
Rating: 5.0 (6 reviews)

Cat. No.: HY-12014 Purity: 98.82%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

SU11274 Chemical Structure

CAS No. : 658084-23-2

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Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 206	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 206	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 121	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 187	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 374	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 605	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 935	In-stock	Estimated Time of Arrival: December 31
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Based on 6 publication(s) in Google Scholar

6 Publications Citing Use of MCE SU11274

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Biological Activity
Protocol
Purity & Documentation
References
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Description

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	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.

Molecular Weight

568.09

Formula

C₂₈H₃₀ClN₅O₄S

CAS No.

658084-23-2

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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: ≥ 2.5 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
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μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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.

Purity & Documentation

Purity: 98.82%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (259 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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]

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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

SU11274 Related Classifications

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:

SU11274658084-23-2PKI-SU11274SU 11274SU-11274c-Met/HGFRAutophagyApoptosisInhibitorinhibitorinhibit

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SU11274 (Synonyms: PKI-SU11274)

Customer Review

SU11274 Related Antibodies

6 Publications Citing Use of MCE SU11274

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Customer Review

SU11274 Related Antibodies

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Complete Stock Solution Preparation Table

SU11274 Related Classifications

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