SMILES string
CC1=CC(C)=CC(NC2=NC=CC(C3=NC(C)=C(C(N[C@@H](C)CO)=O)S3)=N2)=C1
assay
≥99% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 50 mg/mL, pale yellow
shipped in
ambient
storage temp.
−20°C
Quality Level
General description
A cell-permeable 4-thiazolyl-2-phenylaminopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of spleen tyrosine kinase (Syk) (Ki = 9nM). Exhibits excellent selectivity over Cdk2 (Ki ≥ 3.33 µM); ROCK Ki = 2.3 µM), Src Ki ≥ 3.33 µM) and ZAP 70 (Ki = 240 nM). Shown to inhibit mast cell degranulation (IC50 = 70 nM) that is commonly observed in asthma and other allergic diseases.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°c.
Other Notes
Farmer, L., et al. 2008. Bioorg. Med. Chem. Lett.18, 6231.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Priyanka Ramesh et al.
Pharmaceutics, 13(11) (2021-11-28)
Rearranged during transfection (RET) is a tyrosine kinase oncogenic receptor, activated in several cancers including non-small-cell lung cancer (NSCLC). Multiple kinase inhibitors vandetanib and cabozantinib are commonly used in the treatment of RET-positive NSCLC. However, specificity, toxicity, and reduced efficacy
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