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Description: G-749 (G749) is a novel and potent FLT3 inhibitor with potential antineoplastic activity. It inhibits FLT3 (WT), FLT3 (D835Y), and Mer with IC50s of 0.4 nM, 0.6 nM and 1 nM, respectively. G-749 demonstrates high anti-proliferative activity in vitro and in vivo antitumor efficacy as well. G-749 retained its inhibitory potency in various drug-resistance milieus such as patient plasma, FLT3 ligand surge, and stromal protection.
References: Blood. 2014 Apr 3; 123(14):2209-19.
Chemical Name: 8-bromo-2-((1-methylpiperidin-4-yl)amino)-4-((4-phenoxyphenyl)amino)pyrido[4, 3-d]pyrimidin-5(6H)-one
InChi Key: SXWMIXPJPNCXQQ-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H25BrN6O2/c1-32-13-11-17(12-14-32)29-25-30-22-20(26)15-27-24(33)21(22)23(31-25)28-16-7-9-19(10-8-16)34-18-5-3-2-4-6-18/h2-10, 15, 17H, 11-14H2, 1H3, (H, 27, 33)(H2, 28, 29, 30, 31)
SMILES Code: O=C1NC=C(Br)C2=NC(NC3CCN(C)CC3)=NC(NC4=CC=C(OC5=CC=CC=C5)C=C4)=C21
G-749; G 749; G749
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