SU11274 (PKI SU11274; PKI SU11274)

Alias: SU-11274; PKI-SU11274; PKI SU11274; PKI-SU11274;SU 11274; SU11274
Cat No.:V0592 Purity: ≥98%
SU11274 (also called PKI-SU11274; PKI-SU-11274) is a novel, potent and selective Met inhibitor with potential antineoplastic activity.
SU11274 (PKI SU11274; PKI SU11274) Chemical Structure CAS No.: 658084-23-2
Product category: c-MET
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

SU11274 (also called PKI-SU11274; PKI-SU-11274) is a novel, potent and selective Met inhibitor with potential antineoplastic activity. It has no effect on PGDFRβ, EGFR, or Tie2, and in cell-free assays, it inhibits Met with an IC50 of 10 nM. SU11274 effectively inhibits the growth and migration of pancreatic cancer cells. Furthermore, it amplifies the DU145 prostate cancer cell line's reaction to ionizing radiation. With IC50 values ranging from 0.8 to 4.4 μM, SU11274 suppresses the phosphorylation of c-Met induced by hepatocyte growth factor and its subsequent signaling in c-Met-expressing non-small cell lung cancer (NSCLC) cells.

Biological Activity I Assay Protocols (From Reference)
Targets
Met (IC50 = 10 nM)
ln Vitro

SU11274 demonstrates selectivity against other tyrosine kinases, including FGFR-1, c-src, PDGFbR, and EGFR, of over 500 times and more than 50 times, respectively, for Met relative to Flk. Key PI3K pathway regulators such as AKT, FKHR, or GSK3β are inhibited from being phosphorylated by SU11274. Without affecting the growth of BaF3 cells transformed by other oncogenic tyrosine kinases, such as BCR-ABL, TEL-JAK2, TEL-ABL, and TEL-PDGFβR, SU11274 treatment inhibits the growth of TPR-MET-transformed BaF3 cells in a dose-dependent manner with an IC50 of less than 3 μM in the absence of interleukin 3. Apart from growth, BaF3 TPR-MET cells' migration is significantly inhibited by SU11274 treatment, with reductions of 44.8% and 80% at 1 μM and 5 μM, respectively. SU11274 has an IC50 of 1-1.5 μM and suppresses HGF-dependent cell motility and proliferation as well as the phosphorylation of Met. SU11274 inhibits HGF-induced cell growth in H69 and H345 cells, which have functional Met receptors. The inhibitory concentrations are 3.4 μM and 6.5 μM, respectively. SU11274 causes a 24% caspase-dependent apoptosis at 1 μM and a 42.4% increase in G1 phase cells at 5 μM, resulting in G1 cell cycle arrest[2]. SU11274 impedes the viability of c-Met-expressing non-small cell lung cancer (NSCLC) cells, with IC50 values ranging from 0.8 to 4.4 μM. Additionally, it prevents the phosphorylation of c-Met induced by hepatocyte growth factor and its subsequent signaling[3].

ln Vivo

Enzyme Assay
The human c-Met cytoplasmic domain is fused to glutathione S-transferase (GST) to create a chimeric protein that is expressed in SF9 cells. An ELISA-based Met biochemical assay employing the random copolymer poly(Glu:Tyr) (4:1) immobilized on microtiter plates as a substrate makes use of the c-Met kinase GST-fusion protein. In a buffer containing 5 μM ATP, 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate, the IC50 value is calculated using different concentrations of SU11274. The kinase reaction is run at room temperature for five minutes. Using anti-pTyr antibodies conjugated with horseradish peroxidase, the degree of substrate phosphorylation is quantified.
Cell Assay
For 24, 48, and 72 hours, cells are exposed to different SU11274 concentrations with or without HGF. Trypan blue exclusion or the MTT assay are used to count the number of viable cells. Using propidium iodide staining and Annexin V-positive staining, respectively, fluorescence-activated cell sorter analysis measures the cell cycle and apoptosis.
Animal Protocol


References

[1]. 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.

[2]. 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.

[3]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C28H30CIN5O4S
Molecular Weight
568.09
Exact Mass
567.17
Elemental Analysis
C, 59.20; H, 5.32; Cl, 6.24; N, 12.33; O, 11.27; S, 5.64
CAS #
658084-23-2
Appearance
Solid powder
SMILES
CC1=C(NC(=C1C(=O)N2CCN(CC2)C)C)/C=C\3/C4=C(C=CC(=C4)S(=O)(=O)N(C)C5=CC(=CC=C5)Cl)NC3=O
InChi Key
FPYJSJDOHRDAMT-KQWNVCNZSA-N
InChi Code
InChI=1S/C28H30ClN5O4S/c1-17-25(30-18(2)26(17)28(36)34-12-10-32(3)11-13-34)16-23-22-15-21(8-9-24(22)31-27(23)35)39(37,38)33(4)20-7-5-6-19(29)14-20/h5-9,14-16,30H,10-13H2,1-4H3,(H,31,35)/b23-16-
Chemical Name
(3Z)-N-(3-chlorophenyl)-3-[[3,5-dimethyl-4-(4-methylpiperazine-1-carbonyl)-1H-pyrrol-2-yl]methylidene]-N-methyl-2-oxo-1H-indole-5-sulfonamide
Synonyms
SU-11274; PKI-SU11274; PKI SU11274; PKI-SU11274;SU 11274; SU11274
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~92 mg/mL (~161.9 mM)
Water: <1 mg/mL
Ethanol: ~2 mg/mL (~3.5 mM)
Solubility (In Vivo)
30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • SU11274

  • SU11274
  • SU11274
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