G9420

GNF-2

≥98% (HPLC), solid

• Synonym(s): 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide
• Empirical Formula (Hill Notation): C₁₈H₁₃F₃N₄O₂
• CAS Number: 778270-11-4
• Molecular Weight: 374.32
• MDL number: MFCD09265253
• UNSPSC Code: 12352200
• PubChem Substance ID: 24724498
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• form: solid
• color: off-white
• solubility: H₂O: <2 mg/mL; DMSO: ≥5 mg/mL
• storage temp.: 2-8°C
• SMILES string: NC(=O)c1cccc(c1)-c2cc(Nc3ccc(OC(F)(F)F)cc3)ncn2
• InChI: 1S/C18H13F3N4O2/c19-18(20,21)27-14-6-4-13(5-7-14)25-16-9-15(23-10-24-16)11-2-1-3-12(8-11)17(22)26/h1-10H,(H2,22,26)(H,23,24,25)
• InChI key: WEVYNIUIFUYDGI-UHFFFAOYSA-N

Description

Biochem/physiol Actions

GNF-2 belongs to a new class of Bcr-abl inhibitors. GNF-2 appears to bind to the myristoyl binding pocket, an allosteric site distant from the active site, stabilizing the inactive form of the kinase. It inhibits Bcr-abl phosphorylation with an IC₅₀ of 267 nM, but does not inhibit a panel of 63 other kinases, including native c-Abl, and shows complete lack of toxicity towards cells not expressing Bcr-Abl. GNF-2 shows great potential for a new class of inhibitor to study Bcr-abl activity and to treat resistant Chronic myelogenous leukemia (CML), which is caused the Bcr-Abl oncoprotein.

Features and Benefits

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound is featured on the Abl page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Personal Protective Equipment: dust mask type N95 (US), Eyeshields, Gloves