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Chemical Structure| 658084-23-2 Chemical Structure| 658084-23-2

Structure of SU11274
CAS No.: 658084-23-2

Chemical Structure| 658084-23-2

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

Synonyms: PKI-SU11274; Met Kinase Inhibitor

4.5 *For Research Use Only !

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Product Details of SU11274

CAS No. :658084-23-2
Formula : C28H30ClN5O4S
M.W : 568.09
SMILES Code : C(=C\1/C=2C(NC1=O)=CC=C(S(N(C)C3=CC(Cl)=CC=C3)(=O)=O)C2)\C4=C(C)C(C(=O)N5CCN(C)CC5)=C(C)N4
Synonyms :
PKI-SU11274; Met Kinase Inhibitor
MDL No. :MFCD08276928

Safety of SU11274

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of SU11274

epigenetics
RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
hepatocytes 1 μM inhibition of c-met signaling reduced β2AR-mediated upregulation of cell cycle markers and cell proliferation PMC9237079
SKMES1 cells 20 nM SU11274 significantly inhibited HGF-induced migration of SKMES1 cells PMC4551384
A549 cells 20 nM SU11274 significantly inhibited HGF-induced migration of A549 cells PMC4551384
HK-2 cells 1, 5, 10 μM 18 hours Inhibition of c-Met phosphorylation attenuated the cytoprotective effect of GM6001 under hypoxia PMC7228646
RAW264.7 cells 0.5 μM 5 days SU11274 blocked the catalytic effect of HGF on osteoclast differentiation PMC7732867
BμMs cells 0.5 μM 5 days SU11274 blocked the catalytic effect of HGF on osteoclast differentiation PMC7732867
A549 cells 5 μmol/l 4 hours Inhibited HGF-induced c-Met phosphorylation, thereby suppressing the activation of Akt/mTOR/S6 signaling pathway PMC4972091
PC-9 cells 5 μmol/l 4 hours Inhibited HGF-induced c-Met phosphorylation, thereby suppressing the activation of Akt/mTOR/S6 signaling pathway PMC4972091
MDA-MB-231 10 µM 72 hours To determine the synthetic lethal effect of SU11274 with gefitinib, results showed that the combination of SU11274 and gefitinib significantly reduced the viability of MDA-MB-231 cells. PMC4735702
HS578T 10 µM 72 hours To evaluate the effect of the combination of SU11274 and gefitinib on HS578T cells, results showed that the combination significantly reduced cell viability. PMC4735702

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Pulmonary fibrosis model Intraperitoneal injection 0.36–0.50 mg/kg Single injection To investigate the effect of SU11274 on the anti-pulmonary fibrosis effect of curcumin, results showed that SU11274 almost completely abolished the anti-fibrotic effect of curcumin. PMC8027789
C57BL/6 mice Collagen-induced arthritis (CIA) model Intraperitoneal injection 10 mg/kg three or five times per week for two weeks SU11274 significantly increased the bone mass of trabecular bone in CIA mice PMC7732867
Rat Acute Lung Injury Model Intraperitoneal injection 0.18 mg/kg Once daily for 21 days To observe the effect of SU11274 on the proliferation of AEC2s after acute lung injury, the results showed that SU11274 significantly reduced the number of AEC2s. PMC5141641

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.80mL

1.76mL

0.88mL

17.60mL

3.52mL

1.76mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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