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SU11274

Cat. No. M1890

SU11274 Structure

Synonym: PKI-SU11274

Size Price Availability Quantity
10mg USD 158 In stock
50mg USD 568 In stock
100mg USD 720 In stock
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Quality Control
Biological Activity

SU11274 (PKI-SU11274) is a Met kinase inhibitor with IC50 of 10 nM. c-Met is a prognostic marker and potential therapeutic target in clear cell renal cell carcinoma. c-Met protein was activated in all cell lines, and SU11274 can block proliferation (and colony formation). c-Met inhibition could significantly suppress cell survival and proliferation as well as enhance the radiosensitivity of DU145 cells. SU11274 on DU145 cells may include the inhibition of c-Met signaling, depolarization of the mitochondrial membrane potential, impairment of DNA repair function, abrogation of cell cycle arrest, and enhancement of cell death.

Protocol
Cell Experiment
Cell lines LoVo cells line
Preparation method MTT assay.
After pancreatic enzymeization, cells were seeded in 96-well plates at 1 9 105/ml (200 ll/well) and allowed to adhere overnight. SU11274, dissolved in 1 % DMSO and diluted in medium, was added at different concentrations 0.1, 0.5, 2.5 μM, 2μl per well. Another 4 wells were set as a reference and incubated for 24, 48 and 72 h. Twenty microliter MTT (5 g/l; Invitrogen, USA) was added, and cells were incubated for another 4 h. The supernatant was removed, 150 ll DMSO was added and oscillated for 10 min avoiding light at room temperature. The assessment procedure was repeated 3 times, and the average value was determined from each well as the absorbance value at 490 nm on a microplate reader.
Concentrations 0.1, 0.5, 2.5 μM
Incubation time 24, 48 and 72 h
Animal Experiment
Animal models LoVo cells tumor xenograft in 4- to 5-week-old female nude mice (BALB/c-nu/nu)
Formulation 1 % DMSO
Dosages 0.18, 0.09, 0.0225 mg/kg once daily for 30 days from the day that the tumors became palpable
Administration celiac injection
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 568.09
Formula C28H30ClN5O4S
CAS Number 658084-23-2
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
References

Study of critical role of c-Met and its inhibitor SU11274 in colorectal carcinoma.
Gao W, et al. Med Oncol. 2013 Jun;30(2):546. PMID: 23536000.

c-Met inhibitor SU11274 enhances the response of the prostate cancer cell line DU145 to ionizing radiation.
Yu H, et al. Biochem Biophys Res Commun. 2012 Sep 28. PMID: 23026049.

c-Met is a prognostic marker and potential therapeutic target in clear cell renal cell carcinoma.
Gibney GT, et al. Ann Oncol. 2012 Sep 28. PMID: 23022995.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SU11274, PKI-SU11274 supplier, c-Met, inhibitors

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