GNF-2

• Catalog No.: G9420
• CAS Number: 778270-11-4
• M. F.: C18H13F3N4O2
• M. W.: 374.3166296
• Purity: ≥98% (HPLC)

SYNONYMS

• IUPAC name: 3-(6-{[4-(trifluoromethoxy)phenyl]amino}pyrimidin-4-yl)benzamide
• IUPAC Traditional name: 3-(6-{[4-(trifluoromethoxy)phenyl]amino}pyrimidin-4-yl)benzamide
• Synonyms: 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide

DATABASE IDS

• CAS Number: 778270-11-4
• MDL Number: MFCD09265253
• PubChem SID: 24724498

PROPERTIES

• Empirical Formula (Hill Notation): C18H13F3N4O2
• Purity: ≥98% (HPLC)
• Apperance: off-white solid
• Solubility: H2O: <2 mg/mL
• Solubility: DMSO: ≥5 mg/mL
• GHS Signal Word: Warning
• GHS Hazard statements: H315-H319-H335
• European Hazard Symbols: Irritant (Xi)
• Personal Protective Equipment: dust mask type N95 (US), Eyeshields, Gloves
• GHS Precautionary statements: P261-P305 + P351 + P338
• Risk Statements: 36/37/38
• Safety Statements: 26
• Storage Temperature: 2-8°C
• German water hazard class: 3

DETAILS

Description (English)

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.

Description (简体中文)

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.