GNF-5|cas 778277-15-9|DC Chemicals

Cas No.:	778277-15-9
Chemical Name:	Gnf-5
Synonyms:	N-(2-Hydroxyethyl)-3-(6-((4-(trifluoromethoxy)phenyl)amino)pyrimidin-4-yl)benzamide;GNF-5;GNF 5;N-(2-hydroxyethyl)-3-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide;Benzamide, N-(2-hydroxyethyl)-3-(6-((4-(trifluoromethoxy)phenyl)amino)-4-pyrimidinyl)-;CHEBI:806423;CHEMBL1257423;N-(2-hydroxyethyl)-3-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzamide;QC-4300;SureCN924071;UNII-3ZUA56XMQQ;GNF5;3ZUA56XMQQ;N-(2-Hydroxyethyl)-3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide;N-(2-hydroxyethyl)-3-(6-{[4-(trifluoromethoxy)phenyl]amino}pyrimidin-4-yl)benzamide;IIQUYGWWHIHOCF-UHF
SMILES:	FC(OC1C([H])=C([H])C(=C([H])C=1[H])N([H])C1C([H])=C(C2C([H])=C([H])C([H])=C(C(N([H])C([H])([H])C([H])([H])O[H])=O)C=2[H])N=C([H])N=1)(F)F
Formula:	C₂₀H₁₇F₃N₄O₃
M.Wt:	418.3692
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

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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