GNF-5 ,

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100 Gram	FOB Price: USD 1.0000

100 Gram

FOB Price: USD 1.0000

Min.Order :100 Gram
Purity: 98%
Payment Terms : L/C

Keywords

GNF-5 , GNF 5;GNF5;GNF-5;N-(2-Hydroxyethyl)-3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide;ert-butyl 2-oxopiperidine-1-carboxylate;GNF 5 N-(2-Hydroxyethyl)-3-[6-[[4-(trifluoromethoxy)phenyl] 778277-15-9

Quick Details

Appearance:white solid
Application:CAS：778277-15-9； Small molecule inhibitors
PackAge:100g,500g,1kg,25kg/drum
ProductionCapacity:1000|Gram|Week
Storage:Dry seal
Transportation:shipping

Superiority:

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Details:

GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22±0.1 uM (Wild type Abl).
IC50 Value: 0.22±0.1 uM (Wild type Abl) [1]
Target: Abl
GNF-5 is a cell-permeable GNF-2 N-hydroxyethyl carboxamide analog that exhibits in vivo efficacy in suppressing the proliferation of Bcr-abl-expressing Ba/F3 (93% and 83% of no-treatment control, respectively, on days 5 and 7 post treatment; 100 mg/kg b.i.d.) and bone marrow cells (~75% of no-treatment control in both WBC counts and spleen weight on day 7 post treatment; 50 mg/kg b.i.d.) in murine xenograft models of leukemia. Similar to GNF-2, GNF-5 exerts its effect via an allosteric mechanism (IC50 = 0.22 M against wild-type Abl) by targeting the myristate-binding pocket near the c-terminus of Abl kinase domain and thereby altering the conformational dynamics of the ATP-binding pocket. GNF-5 is ineffective toward the myristate-binding site mutant E505K and the ATP-binding site 'gatekeeper' mutant T315I.

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