1370466-81-1
| 中文名称 | 1370466-81-1 |
|---|---|
| 中文同义词 | 化合物 T14937;化合物 CG-806;1-(3-氟-4-(7-(4-甲基-1H-咪唑-2-基)-1-氧代异吲哚啉-4-基)苯基)-3-(3-(三氟甲基)苯基)脲 |
| 英文名称 | CG-806 |
| 英文同义词 | CG-806;Urea, N-[4-[2,3-dihydro-7-(5-methyl-1H-imidazol-2-yl)-1-oxo-1H-isoindol-4-yl]-3-fluorophenyl]-N'-[3-(trifluoromethyl)phenyl]-;N-[4-[2,3-Dihydro-7-(5-methyl-1H-imidazol-2-yl)-1-oxo-1H-isoindol-4-yl]-3-fluorophenyl]-N'-[3-(trifluoromethyl)phenyl]-urea;CG 806,CG806 |
| CAS号 | 1370466-81-1 |
| 分子式 | C26H19F4N5O2 |
| 分子量 | 509.45 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1370466-81-1.mol |
| 结构式 |  |
1370466-81-1 性质
| 沸点 | 686.2±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.465±0.06 g/cm3(Predicted) |
| 酸度系数(pKa) | 10.28±0.20(Predicted) |
FLT3/BTK.
In FLT3-ITD AML cells, CG-806 induces apoptosis through inhibition of FLT3 signaling (decreases phospho-FLT3, -STAT5 and -ERK) and promotion of G0/G1 cell cycle arrest. In FLT3-WT AML cell lines, or Ba/F3 cells transfected with FLT3-WT, D835Y, ITD+D835Y, or ITD+F691L, CG-806 markedly decreases phosphorylation of BTK, aurora kinases (AURK) and H3S10, resulting in G2/M arrest or polyploidy, and apoptosis with less or no effect on FLT3-WT activity. CG-806 decreases BTK phosphorylation in all malignant B cell lines tested and inhibits cell proliferation and colony formation.CG-806 equivalently inhibits BTK-WT and BTK-C481S in HEK293 transfected cells.
CG-806 (0-120 mg/kg; oral administration; for 28 days; CD-1 mice) treatment suppresses leukemia growth at all doses tested throughout the 28-day period of dosing, and has no adverse CG-806-related effects on body weight, ophthalmic, respiratory or neurological examinations, clinical pathology (coagulation, clinical chemistry, or urinalysis), organ weight or macroscopic evaluations in the subcutaneous MV4-11 xenograft model.
| Animal Model: | CD-1 mice with MV4-11 |
| Dosage: | 0 mg/kg, 30 mg/kg, 60 mg/kg or 120 mg/kg |
| Administration: | Oral administration; for 28 days |
| Result: | Suppressed leukemia growth at all doses tested throughout the 28-day period of dosing. |