AS1810722

Name Value
Weight 477.519 g/mol
Zinc ID ZINC53184514
Smiles NC(=O)CN1CCN(c2ccc(Nc3ncc4ccn(Cc5cc(F)cc(F)c5)c4n3)cc2)CC1
Molecular formula C25H25F2N7O
Mode of inhibition STAT and IL-4; Non-peptide small molecule
CAS N/A

Clinical Trials

Study title Status Conditions Link

References

Publication DOI Pubmed PMCID
Novel 7H-pyrrolo[2,3-d]pyrimidine derivatives as potent and orally active STAT6 inhibitors. Bioorganic & medicinal chemistry Shinya Nagashima, Takeshi Hondo, Hiroshi Nagata, Takashi Ogiyama, Jun Maeda, Hiroaki Hoshii, Toru Kontani, Sadao Kuromitsu, Keiko Ohga, Masaya Orita, Kazuki Ohno, Ayako Moritomo, Koichi Shiozuka, Masako Furutani, Makoto Takeuchi, Mitsuaki Ohta, Shin-ichi Tsukamoto, 17, 19, 2009-10-01, 2009-08-15, 10.1016/j.bmc.2009.08.021 10.1016/j.bmc.2009.08.021 19747833 19747833

Vendors

Company Lnk to product
MERCK (Sigma Aldrich) https://www.sigmaaldrich.com/catalog/product/sigma/a6733?lang=pl&region=PL
Tocris https://www.tocris.com/products/auranofin_4600
Caymanchemical https://www.caymanchem.com/product/15316/auranofin
MedChemExpress https://medkoo.com/products/11353
MedChemExpress https://www.medchemexpress.com/Auranofin.html

Filter data

Compound AS1810722
Experiment types Differential cell count, ELISA, LC-MS; HPLC, Western Blot
Concentrations 0.03, 0.10, 0.20, 0.30, 0.50, 1.00, 10.00, 2.00, 3.00, 5.00
Cell lines Astrocytes, HLM, HUVECS, HepG2, Th1, Th2, eosinophil, fibroblast-like synoviocytes (FLS)
Organisms Homo sapiens, Homo sapiens (patient), Mus musculus, Rattus norvegicus
Animal models BALB/c, Sprague–Dawley, c57BL/6
STAT proteins STAT3, p-STAT3, p-STAT3(cytoplasm), p-STAT3(nuclear)
Other IFNγ, IL-4, JAK1, Midazolam metabolites, p-JAK1, β-actin, β-actin (cytoplasm), β-actin (nuclear)

Experiments

Compound Experiment type Investigated event Concentration Cell line Organism Animal model Stat protein Details
AS1810722 Western Blot Influence on protein activity in presence of IL-6 2.00 µM HepG2 Homo sapiens p-STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 2.00 µM HepG2 Homo sapiens STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 2.00 µM HepG2 Homo sapiens
AS1810722 Western Blot Influence on protein activity in presence of IL-6 2.00 µM HepG2 Homo sapiens
AS1810722 Western Blot Influence on protein activity in presence of IL-6 2.00 µM HepG2 Homo sapiens
AS1810722 Western Blot Influence on protein activity in presence of IL-6 1.00 µM HepG2 Homo sapiens p-STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 3.00 µM HepG2 Homo sapiens p-STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 1.00 µM HepG2 Homo sapiens STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 3.00 µM HepG2 Homo sapiens STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 1.00 µM HepG2 Homo sapiens
AS1810722 Western Blot Influence on protein activity in presence of IL-6 3.00 µM HepG2 Homo sapiens
AS1810722 Western Blot Influence on protein activity in presence of IL-6 1.00 µM HepG2 Homo sapiens
AS1810722 Western Blot Influence on protein activity in presence of IL-6 3.00 µM HepG2 Homo sapiens
AS1810722 Western Blot Influence on protein activity in presence of IL-6 1.00 µM HepG2 Homo sapiens
AS1810722 Western Blot Influence on protein activity in presence of IL-6 3.00 µM HepG2 Homo sapiens
AS1810722 Western Blot Influence on protein activity in presence of IL-6 2.00 µM HepG2 Homo sapiens p-STAT3(nuclear)
AS1810722 Western Blot Influence on protein activity in presence of IL-6 2.00 µM HepG2 Homo sapiens p-STAT3(cytoplasm)
AS1810722 Western Blot Influence on protein activity in presence of IL-6 2.00 µM HepG2 Homo sapiens
AS1810722 Western Blot Influence on protein activity in presence of IL-6 2.00 µM HepG2 Homo sapiens
AS1810722 Western Blot Influence on protein activity in presence of IL-6 2.00 µM HepG2 Homo sapiens
AS1810722 Western Blot Influence on protein activity in presence of IL-6 0.10 µM fibroblast-like synoviocytes (FLS) Homo sapiens (patient) p-STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 0.30 µM fibroblast-like synoviocytes (FLS) Homo sapiens (patient) p-STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 0.50 µM fibroblast-like synoviocytes (FLS) Homo sapiens (patient) p-STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 1.00 µM fibroblast-like synoviocytes (FLS) Homo sapiens (patient) p-STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 0.10 µM fibroblast-like synoviocytes (FLS) Homo sapiens (patient) STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 0.30 µM fibroblast-like synoviocytes (FLS) Homo sapiens (patient) STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 0.50 µM fibroblast-like synoviocytes (FLS) Homo sapiens (patient) STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 1.00 µM fibroblast-like synoviocytes (FLS) Homo sapiens (patient) STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 in tissue 0.20 µM Astrocytes Rattus norvegicus Sprague–Dawley p-STAT3
AS1810722 Western Blot Influence on protein activity in presence of IL-6 in tissue 0.20 µM Astrocytes Rattus norvegicus Sprague–Dawley STAT3
AS1810722 Western Blot Influence on protein activity in presence of FBS 0.10 µM HUVECS Homo sapiens (patient)
AS1810722 Western Blot Influence on protein activity in presence of FBS 0.30 µM HUVECS Homo sapiens (patient)
AS1810722 Western Blot Influence on protein activity in presence of FBS 0.50 µM HUVECS Homo sapiens (patient)
AS1810722 LC-MS; HPLC Influence on hepatic metabolism 5.00 µM HLM Homo sapiens
AS1810722 ELISA Influence on cell differentiation 0.10 nM Th1 Mus musculus c57BL/6
AS1810722 ELISA Influence on cell differentiation 0.10 nM Th2 Mus musculus c57BL/6
AS1810722 ELISA Influence on cell differentiation 1.00 nM Th1 Mus musculus c57BL/6
AS1810722 ELISA Influence on cell differentiation 1.00 nM Th2 Mus musculus c57BL/6
AS1810722 ELISA Influence on cell differentiation 10.00 nM Th1 Mus musculus c57BL/6
AS1810722 ELISA Influence on cell differentiation 10.00 nM Th2 Mus musculus c57BL/6
AS1810722 Differential cell count Influence on eosinophils accumulation in BALF 0.03 mg/kg eosinophil Mus musculus BALB/c
AS1810722 Differential cell count Influence on eosinophils accumulation in BALF 0.10 mg/kg eosinophil Mus musculus BALB/c
AS1810722 Differential cell count Influence on eosinophils accumulation in BALF 0.30 mg/kg eosinophil Mus musculus BALB/c