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HomeProduct name listGNF-2

GNF-2

Synonym(s):(3-(6)-(4-Trifluoromethoxy-phenylamino)-pyrimidin-4-yl)-benzamide, GNF-2, Abl Inhibitor I;3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide;Bcr-abl Inhibitor - CAS 778270-11-4 - Calbiochem

  • CAS NO.:778270-11-4
  • Empirical Formula: C18H13F3N4O2
  • Molecular Weight: 374.32
  • MDL number: MFCD09265253
  • EINECS: 200-256-5
  • SAFETY DATA SHEET (SDS)
  • Update Date: 2024-10-31 18:15:48
GNF-2 Structural

What is GNF-2?

Description

GNF-2 is an allosteric inhibitor of Bcr-Abl (IC50 = 267 nM). It is selective for Bcr-Abl over c-Abl and a panel of 63 additional kinases at 10 μM. It inhibits proliferation of Ba/F3 cells (IC50 = 138 nM). GNF-2 (10 μM) reduces viral titers in Vero cells infected with infectious bronchitis virus (IBV), a coronavirus, via inhibition of IBV surface glycoprotein-induced syncytia formation and virus-cell fusion. It inhibits LPS-induced production of nitric oxide (NO) and TNF-α in BV-2 microglia when used at concentrations of 10 and 20 μM. GNF-2 (1 and 10 mg/kg) reduces paw edema and increases the latency to paw withdrawal in a mouse model of inflammatory pain induced by complete Freund’s adjuvant (CFA). It also decreases mechanical and thermal hyperalgesia in a mouse model of diabetic neuropathy induced by streptozotocin (STZ; ).

The Uses of GNF-2

Bcr-abl Inhibitor is an inhibitor of c-Abl and Bcr-abl activity. It is a COVID19-related research product.

What are the applications of Application

Bcr-abl Inhibitor is an inhibitor of c-Abl and Bcr-abl activity

Definition

ChEBI: 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide is a member of pyrimidines.

General Description

A cell-permeable and reverisble pyrimidine compound that binds to the c-abl myristoyl binding pocket and acts as an allosteric, non-ATP-competitive inhibitor of cellular Bcr-abl activity and Bcr-abl-dependent cellular functions. Exhibits little inhibitory effect against a panel of 63 kinases even at concentration as high as 10 μM. Exhibits potent and selective antiproliferative activity toward Bcr-abl-expressing cells (IC50 = 138 nM, 194 nM, 268 nM and 273 nM in Ba/F3.p210, Ba/F3.p185Y253H, SUP-B15 and Ba/F3.p210E255V, and K562, respectively). Brij-35 is reported to mask the inhibitory effect of GNF-2 in cell-free c-abl and Bcr-abl kinase assays.

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.

Properties of GNF-2

storage temp.  2-8°C
solubility  H2O: <2mg/mL
form  White solid
color  off-white

Safety information for GNF-2

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for GNF-2

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