8-Bromo-2-((1-Methylpiperidin-4-Yl)Amino)-4-((4-Phenoxyphenyl)Amino)Pyrido[4,3-D]Pyrimidin-5(6H)-One 8-溴-2-((1-甲基哌啶-4-基)氨基)-4-((4-苯氧基苯基)氨基)吡啶并[4,3-d]嘧啶-5(6H)-酮
CAS 1457983-28-6 MFCD557983286
化学结构图
SMILES: CN1CCC(Nc2nc(Nc3ccc(Oc4ccccc4)cc3)c3c(=O)[nH]cc(Br)c3n2)CC1
化学属性
| Mol. Weight | 521.41 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | 8-Bromo-2-((1-Methylpiperidin-4-Yl)Amino)-4-((4-Phenoxyphenyl)Amino)Pyrido[4,3-D]Pyrimidin-5(6H)-One |
|---|---|
| Formula | C25H25BrN6O2 |
| Synonym | G749; G-749; G 749 |
| IUPAC Name | 8-bromo-2-((1-methylpiperidin-4-yl)amino)-4-((4-phenoxyphenyl)amino)pyrido[4,3-d]pyrimidin-5(6H)-one |
| InChIKey | SXWMIXPJPNCXQQ-UHFFFAOYSA-N |
| InChI | 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) |
| Canonical SMILES | O=C1NC=C(Br)C2=NC(NC3CCN(C)CC3)=NC(NC4=CC=C(OC5=CC=CC=C5)C=C4)=C21 |
| Chemical Name Translation | 8-溴-2-((1-甲基哌啶-4-基)氨基)-4-((4-苯氧基苯基)氨基)吡啶并[4,3-d]嘧啶-5(6H)-酮 |
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产品应用
- G-749 is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants including FLT3-ITD, FLT3-D835Y, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays. G-749 retained its inhibitory potency in various drug-resistance milieus such as patient plasma, FLT3 ligand surge, and stromal protection. Furthermore, it displayed potent antileukemic activity in bone marrow blasts from AML patients regardless of FLT3 mutation status, including those with little or only minor responses to AC220 or PKC412. Oral administration of G-749 yielded complete tumor regression and increased life span in animal models. Thus, G-749 appears to be a promising next-generation drug candidate for the treatment of relapsed and refractory AML patients with various FLT3-ITD/FLT3-TKD mutants and further shows the ability to overcome drug resistance (Blood. 2014 Apr 3;123(14):2209-19).
