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SGX-523

CAT: 0013-GTR19164063-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19164063-01Size:200 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
SGX-523 is a potent, selective ATP-competitive inhibitor of MET receptor tyrosine kinase with IC50 of 4 nM, does not inhibit RON and a panel of kinases; shows higher affinity for unphosphorylated form of MET (Ki = 2.7 nM) versus the more active phospho-MET (Ki=23 nM) ; inhibits MET-mediated signaling, cell proliferation, and cell migration at nanomolar concentrations but has no effect on signaling dependent on other protein kinases; inhibits MET autophosphorylation with IC50 of 40 nM in GTL16 cells, inhibits MET-dependent tumor growth in vivo.Solid Tumors Phase 1 Discontinued (In Vitro) :SGX523 shows ATP-competitive inhibition with higher apparent affinity for the less active, unphosphorylated form of MET [MET-KD (0P), Ki=2.7 nM] versus the more active phospho-enzyme [MET-KD (3P), Ki=23 nM].SGX523 inhibits the growth of gastric and lung cancer cell lines with amplification of the MET gene but has no effect, even at high micromolar concentration, on cell lines with normal MET gene copy number. TheIC50s of 0.02, 0.113, and 0.035 μM for NSCLC H1993, gastric cncer MKN45, and gastric cancer Hs746T cells, respectively.The IC50 value for the inhibition of MET autophosphorylation is 0.040 μM in GTL16 cells.SGX523 (0.5, 1.5, 4.6, 13.7, 41, 123, 370, 1100, 3300, 10000 nM; 1 hour) inhibits MET autophosphorylation without affecting total MET or extracellular signal-regulated kinase protein levels in HGF-stimulated A549 cells. (In Vivo) :SGX523 exhibits antitumor activity in vivo. SGX523 inhibits MET-dependent tumor growth.
CAS Number
1022150-57-7
Product Name Alternative
SGX523 | SGX 523
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 3.6 mg/mL
Smiles
CN1N=CC (C2=NN3C (C=C2) =NN=C3SC4=CC=C5N=CC=CC5=C4) =C1
Molecular Formula
C18H13N7S
Molecular Weight
359.4077
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
Quinoline, 6-[[6- (1-methyl-1H-pyrazol-4-yl) -1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]-

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