SU 11274
(3Z)-N-(3-chlorophenyl)-3-({3,5-dimethyl-4-[(4-methylpiperazin-1-yl)carbonyl]-1H-pyrrol-2-yl}methylidene)-N-methyl-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide
CAS: 658084-23-2
Molecular Formula: C28H30ClN5O4S
SU 11274 - Names and Identifiers
SU 11274 - Physico-chemical Properties
| Molecular Formula | C28H30ClN5O4S |
| Molar Mass | 568.09 |
| Density | 1.401±0.06 g/cm3(Predicted) |
| Solubility | DMSO : 100 mg/mL mother liquor preservation: sub-package and freeze storage to avoid repeated freezing and thawing;-20 ℃,1 month;-80 ℃,6 months (after dilution, the solution temperature is low and storage may precipitate, try to use it now) Cell experiment: Dissolve with DMSO first: dilute with culture medium then, and the dilution process is recommended to be carried out in stages to avoid too fast concentration change leading to compound precipitation. If the compound is precipitated during the dilution process, it can be redissolved by ultrasound. During dilution, ensure that the final concentration of DMSO in the working fluid should be below 0.1% as far as possible, and the maximum should not exceed 0.5%, and set up a DMSO control group with corresponding concentration. Animal experiment: Dissolve with DMSO first: dilute with water or normal saline, etc. The dilution process is recommended to be carried out in sections to avoid excessive concentration changes leading to compound |
| Appearance | powder |
| Color | orange |
| pKa | 11.62±0.20(Predicted) |
| Storage Condition | 2-8°C |
| Refractive Index | 1.664 |
| MDL | MFCD08276928 |
| Use | SU11274(IC50=10 nM) is a specific Met inhibitor. It shows no significant effects on PGDFRβ, EGFR or Tie2. |
| Target | CDK2 FGFR1 Flk1 Met RON |
| In vitro study | SU11274 is 50-fold more selective for Met than Flk and 500-1000-fold more selective for other tyrosine kinases, such as FGFR-1, c-src, PDGF BR, and EGFR. SU11274 inhibits phosphorylation of key regulators of the PI3K pathway, including AKT, FKHR, or GSK3β. In the presence of interleukin-3, SU11274 treatment inhibited the growth of transformed BaF3 cells by TPR-MET in a dose-dependent manner with IC50<3 μm, other oncogenic tyrosine kinase-transformed BaF3 cell growth was not inhibited, including BCR-ABL, TEL-JAK2, TEL-ABL, and TEL-PDGFβR. In addition to inhibition of cell growth, SU11274 treatment also significantly inhibited BaF3.TPR-MET cell migration by 44.8% and 80% for 1 μm and 5 μm treatments, respectively. SU11274 inhibits HGF-dependent Met phosphorylation, and HGF-dependent cell proliferation and activity with an IC50 of 1-1.5 μm. SU11274 inhibited HGF-induced cell growth by acting on H69 and H345 cells with functional Met receptors with IC50 of 3.4 μm and 6.5 μm, respectively. 5 M SU11274 treatment, the cell cycle was stopped at G1 phase, the G1 phase cells increased from 42.4% to 70.6%, and induced caspase dependent apoptosis, according to 1 M treatment, apoptosis of 24%. SU1127 acts on non-small cell lung cancer (NSCLC) cells expressing c-Met, inhibits cell viability with an IC50 of 0.8-4.4 μm, and abrogates liver growth factor-induced phosphorylation of c-Met and its downstream signals. |
SU 11274 - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
| WGK Germany | 3 |
SU 11274 - Reference
| Reference Show more | 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):1085-1092.2. 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), 5462-5469.3. 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. |
SU 11274 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.76 ml | 8.801 ml | 17.603 ml |
| 5 mM | 0.352 ml | 1.76 ml | 3.521 ml |
| 10 mM | 0.176 ml | 0.88 ml | 1.76 ml |
| 5 mM | 0.035 ml | 0.176 ml | 0.352 ml |
Last Update：2024-01-02 23:10:35
SU 11274 - Cell Experiment
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. (Only for Reference) Cell lines: BaF3.TPR-MET, H69 and H345 cells
Last Update：2023-08-16 21:32:38
SU 11274 - Reference Information
| biological activity | SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free tests and no effect on PGDFRβ,EGFR and Tie2. SU11274 can induce autophagy, apoptosis and cell cycle arrest. |
| target | TargetValue Met (Cell-free say) 0.01 μM |
| Target | Value |
| Met (Cell-free assay) | 0.01 μM |
| in vitro study | when SU11274 acts on Met, the selectivity is 50 times higher than that when it acts on Flk, and 500-1000 times higher than that when it acts on other tyrosine kinases, such as FGFR-1, c-src, PDGFbR, and EGFR. SU11274 inhibits phosphorylation of key regulators of PI3K pathway, including AKT, FKHR, or GSK3β. In the presence of interleukin-3, SU11274 treatment inhibits the growth of TPR-MET-transformed BaF3 cells. This effect exists in a dose-dependent manner, IC50<3 μM, and does not inhibit the growth of other oncogenic tyrosine kinase-transformed BaF3 cells, including BCR-ABL, TEL-JAK2, TEL-ABL, and TEL-PDGFβR. In addition to inhibiting cell growth, SU11274 treatment also significantly inhibited BaF3.TPR-MET cell migration, with 1 μM and 5 μM treatment inhibiting 44.8% and 80% respectively. SU11274 inhibit HGF-dependent Met phosphorylation and HGF-dependent cell proliferation and activity, IC50 is 1-1.5 μM. SU11274 acts on H69 and H345 cells with functional Met receptors to inhibit HGF-induced cell growth with IC50 of 3.4 μM and 6.5 μM respectively. 5 μM SU11274 treatment stopped the cell cycle in G1 phase, increased G1 phase cells from 42.4% to 70.6%, and induced caspase-dependent apoptosis. According to 1 μM treatment, apoptosis reached 24%. SU1127 acts on non-small cell lung cancer (NSCLC) cells expressing c-Met, inhibits cell viability, IC50 is 0.8-4.4 μM, and abolishes liver growth factor-induced c-Met and its downstream signal phosphorylation. |
Last Update：2024-04-09 20:02:46
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CAS: 658084-23-2
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CAS: 658084-23-2
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Product Name: SU11274 Visit Supplier Webpage Request for quotation
CAS: 658084-23-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 658084-23-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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