Basic information Safety Supplier Related
ChemicalBook >  Product Catalog >  Biochemical Engineering >  Inhibitors >  protein tyrosine kinase >  SGX-523

SGX-523

Basic information Safety Supplier Related

SGX-523 Basic information

Product Name:
SGX-523
Synonyms:
  • SGX-523
  • 6-[[6-(1-Methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]quinoline
  • SGX 523(SGX-523)
  • Quinoline,6-[[6-(1-Methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]-
  • 6-[[6-(1-Methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]quinoline SGX 523
  • SGX-523, >=98%
  • 6-[[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl]quinoline
  • SGX-523;SGX523; SGX 523
CAS:
1022150-57-7
MF:
C18H13N7S
MW:
359.41
Product Categories:
  • Inhibitors
  • API
Mol File:
1022150-57-7.mol
More
Less

SGX-523 Chemical Properties

Density 
1.485
storage temp. 
Store at -20°C
solubility 
≥17.95 mg/mL in DMSO
form 
solid
pka
3.94±0.10(Predicted)
color 
Light yellow to yellow
More
Less

SGX-523 Usage And Synthesis

Uses

SGX523 is a novel, ATP-competitive kinase inhibitor.

Definition

ChEBI: A member of the class of triazolopyridazines that is 6-(1-methylpyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazine-3-thiol in which the thiol hydrogen is replaced by a quinolin-6-yl group.

Biological Activity

sgx-523 is a novel, potent, atp-competitive, and highly-selective hepatocyte growth factor receptor (met) inhibitor with ic50 value of 4 nm [1].sgx523 inhibits met autophosphorylation in gastric cancer cell line gtl16 and human lung carcinoma cell line a549, with ic50 of 40 nm and 12 nm, respectively [1]. additionally, tumor regression was observed in gastic cancer cell line gtl16 and human gbm cell line u87mg derived mouse xenograft models that are treated with sgx-523 by oral gavage [1].sgx523 has been shown to inhibit the phosphorylateion of mek, mapk, akt in brain cancer cell lines including u87, u373, daoy, as well as glioma stem cells 1228. the inhibition of mek in brain cancer cells and stem cells led to cell proliferation, g1/s cell cycle progression, cell migration, and cell invasion [2].

storage

Store at +4°C

References

[1] buchanan sg1, hendle j, lee ps, smith cr, bounaud py, jessen ka, tang cm, huser nh, felce jd, froning kj, peterman mc, aubol be, gessert sf,sauder jm, schwinn kd, russell m, rooney ia, adams j, leon bc, do th, blaney jm, sprengeler pa, thompson da, smyth l, pelletier la, atwell s, holme k,wasserman sr, emtage s, burley sk, reich sh. sgx523 is an exquisitely selective, atp-competitive inhibitor of the met receptor tyrosine kinase with antitumor activity in vivo. mol cancer ther. 2009 dec;8(12):3181-90.
[2] guessous f1, zhang y, dipierro c, marcinkiewicz l, sarkaria j, schiff d, buchanan s, abounader r.an orally bioavailable c-met kinase inhibitor potently inhibits brain tumor malignancy and growth. anticancer agents med chem. 2010 jan;10(1):28-35.

SGX-523Supplier

Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Email
sales@BioChemBest.com
Capot Chemical Co., Ltd
Tel
+86 (0) 571 85 58 67 18
Email
sales@capotchem.com
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Email
info@chemlin.com.cn
Jinan Trio PharmaTech Co., Ltd.
Tel
+86 (531) 88811783
Email
sales@trio-pharmatech.com (International market)
More
Less

SGX-523(1022150-57-7)Related Product Information