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Chemical Structure| 1022150-57-7 Chemical Structure| 1022150-57-7

Structure of SGX-523
CAS No.: 1022150-57-7

Chemical Structure| 1022150-57-7

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SGX-523 is a potent and selective c-Met inhibitor with IC50 of 4 nM.

4.5 *For Research Use Only !

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Product Details of SGX-523

CAS No. :1022150-57-7
Formula : C18H13N7S
M.W : 359.41
SMILES Code : CN1N=CC(C2=NN3C(C=C2)=NN=C3SC4=CC=C5N=CC=CC5=C4)=C1
MDL No. :MFCD16660190
InChI Key :BCZUAADEACICHN-UHFFFAOYSA-N
Pubchem ID :24779724

Safety of SGX-523

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of SGX-523

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
A172 cells 4 nM 24 h Inhibit MET, reduce circFAM53B-mediated oncogenic effects PMC8942547
H1975WT cells 5μM 24 h The same was not seen in H1975WT cells. PMC5283661
H1975L858R cells 5μM 24 h SGX523 only reduced stroma formation in H1975L858R. PMC5283661
H1975L858R/T790M cells 5μM 24 h SGX523 significantly reduced H1975L858R/T790M cell proliferation and decreased ERK phosphorylation. PMC5283661
H1975WT cells 5μM 24 h To assess the effect of SGX-523 on cell proliferation, results showed that SGX-523 had no significant effect on the proliferation of H1975WT cells. PMC5283661
H1975L858R cells 5μM 24 h To assess the effect of SGX-523 on cell proliferation, results showed that SGX-523 had no significant effect on the proliferation of H1975L858R cells. PMC5283661
H1975L858R/T790M cells 5μM 24 h To assess the effect of SGX-523 on cell proliferation, results showed that SGX-523 significantly reduced the proliferation of H1975L858R/T790M cells. PMC5283661

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Partial hepatectomy model Oral gavage 25 mg/kg Starting on the operative day and continued until the time of animal sacrifice To investigate the inhibitory effect of SGX-523 on c-Met and its impact on liver regeneration. Results showed that SGX-523 significantly reduced phosphorylation of c-Met and attenuated GW9662-induced liver regeneration and hepatocyte proliferation. PMC6082852
BALB/c nude mice Xenograft model using the H1975-derived mutant cell lines Oral gavage 60mg/kg Daily for 12 days SGX523 significantly reduced H1975L858R/T790M-derived tumor growth and decreased ERK phosphorylation. In H1975L858R-derived tumors, MET-EGFR interaction was increased by SGX523. There was no significant change in FRET between MET and EGFR in xenograft tissue derived from H1975WT cells. PMC5283661
BALB/c mice Xenograft model derived from H1975L858R/T790M, H1975L858R, and H1975WT cells Oral gavage 60mg/kg Daily for 12 days To assess the effect of SGX-523 on tumor growth, results showed that SGX-523 significantly inhibited tumor growth in H1975L858R/T790M-derived tumors but had no significant effect on H1975L858R and H1975WT-derived tumors. PMC5283661

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.91mL

2.78mL

1.39mL

27.82mL

5.56mL

2.78mL

References

 

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