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MedKoo CAT#: 407257
CAS#: 839706-07-9
Description: GNF-7 is a type-II T315I inhibitor. GNF-7 inhibits Ack1 and germinal center kinase (GCK). GNF-7 displayed significant in vivo efficacy against T315I-Bcr-Abl without appreciable toxicity in a bioluminescent xenograft mouse model using a transformed T315I-Bcr-Abl-Ba/F3 cell line that has a stable luciferase expression. GNF-7 is among the first type-II inhibitors capable of inhibiting T315I to be described and will serve as a valuable lead to design the third generation Bcr-Abl kinase inhibitors.
MedKoo Cat#: 407257
Name: GNF-7
CAS#: 839706-07-9
Chemical Formula: C28H24F3N7O2
Exact Mass: 547.1944
Molecular Weight: 547.5422
Elemental Analysis: C, 61.42; H, 4.42; F, 10.41; N, 17.91; O, 5.84
Synonym: GNF-7; GNF7; GNF 7.
IUPAC/Chemical Name: N-(4-methyl-3-(1-methyl-7-((6-methylpyridin-3-yl)amino)-2-oxo-1,4-dihydropyrimido[4,5-d]pyrimidin-3(2H)-yl)phenyl)-3-(trifluoromethyl)benzamide
InChi Key: SZNYUUZOQHNEKB-UHFFFAOYSA-N
InChi Code: InChI=1S/C28H24F3N7O2/c1-16-7-9-21(34-25(39)18-5-4-6-20(11-18)28(29,30)31)12-23(16)38-15-19-13-33-26(36-24(19)37(3)27(38)40)35-22-10-8-17(2)32-14-22/h4-14H,15H2,1-3H3,(H,34,39)(H,33,35,36)
SMILES Code: O=C(NC1=CC=C(C)C(N2CC3=CN=C(NC4=CC=C(C)N=C4)N=C3N(C)C2=O)=C1)C5=CC=CC(C(F)(F)F)=C5
1: Liang X, Liu X, Wang B, Zou F, Wang A, Qi S, Chen C, Zhao Z, Wang W, Qi Z, Lv
F, Hu Z, Wang L, Zhang S, Liu Q, Liu J. Discovery of
2-((3-amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phe
nyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a potent,
selective and orally available BCR-ABL/SRC/p38 kinase inhibitor for Chronic
Myeloid Leukemia. J Med Chem. 2016 Jan 20. [Epub ahead of print] PubMed PMID:
26789553.
2: Lu X, Zhang Z, Ren X, Pan X, Wang D, Zhuang X, Luo J, Yu R, Ding K. Hybrid
pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I)
mutant. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3458-63. doi:
10.1016/j.bmcl.2015.07.006. Epub 2015 Jul 9. PubMed PMID: 26195136.
3: Nonami A, Sattler M, Weisberg E, Liu Q, Zhang J, Patricelli MP, Christie AL,
Saur AM, Kohl NE, Kung AL, Yoon H, Sim T, Gray NS, Griffin JD. Identification of
novel therapeutic targets in acute leukemias with NRAS mutations using a
pharmacologic approach. Blood. 2015 May 14;125(20):3133-43. doi:
10.1182/blood-2014-12-615906. Epub 2015 Apr 1. PubMed PMID: 25833960; PubMed
Central PMCID: PMC4432008.
4: Choi HG, Ren P, Adrian F, Sun F, Lee HS, Wang X, Ding Q, Zhang G, Xie Y, Zhang
J, Liu Y, Tuntland T, Warmuth M, Manley PW, Mestan J, Gray NS, Sim T. A type-II
kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl.
J Med Chem. 2010 Aug 12;53(15):5439-48. doi: 10.1021/jm901808w. PubMed PMID:
20604564; PubMed Central PMCID: PMC4134510.
