1370466-81-1
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- CAS号:
- 1370466-81-1
- 英文名:
- CG-806
- 英文别名:
- CG-806;CG 806,CG806;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;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]-
- 中文名:
- 1370466-81-1
- 中文别名:
- 化合物 T14937
- CBNumber:
- CB64796640
- 分子式:
- C26H19F4N5O2
- 分子量:
- 509.45
- MOL File:
- 1370466-81-1.mol
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1370466-81-1化学性质
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沸点:
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686.2±55.0 °C(Predicted)
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密度:
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1.465±0.06 g/cm3(Predicted)
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酸度系数(pKa):
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10.28±0.20(Predicted)
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1370466-81-1性质、用途与生产工艺
CG-806 是一种口服，有效且非共价的泛-FLT3/泛-BTK 抑制剂，对 FLT3 的 IC50 值为 0.08 µM。CG-806 对 FLT3 野生型转染的 Ba/F3 细胞的 IC50 值为 11 nM。
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.
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Animal Model:
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CD-1 mice with MV4-11
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Dosage:
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0 mg/kg, 30 mg/kg, 60 mg/kg or 120 mg/kg
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Administration:
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Oral administration; for 28 days
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Result:
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Suppressed leukemia growth at all doses tested throughout the 28-day period of dosing.
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1370466-81-1
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1370466-81-1, 1370466-81-1 相关搜索:
- C26H19F4N5O2
- 化合物 T14937
- 1370466-81-1
- CG 806,CG806
- 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
- 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]-
- CG-806