RET激酶抑制剂(AST 487)
AST 487(AST 487)
CAS: 630124-46-8
化学式: C26H30F3N7O2
| 中文名 | AST 487 |
| 英文名 | AST 487 |
| 别名 | 化合物AST 487 RET激酶抑制剂(AST 487) 1-(4-((4-乙基哌嗪-1-基)甲基)-3-(三氟甲基)苯基)-3-(4-((6-(甲基氨基)嘧啶-4-基)氧基)苯基)脲 |
| 英文别名 | CS-562 AST 487 NVP-AST 487 3-{4-[(4-ETHYLPIPERAZIN-1-YL)METHYL]-3-(TRIFLUOROMETHYL)PHENYL}-1-(4-{[6-(METHYLAMINO)PYRIMIDIN-4-YL]OXY}PHENYL)UREA 1-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-(4-((6-(methylamino)pyrimidin-4-yl)oxy)phenyl)urea 1-{4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl}-3-(4-{[6-(methylamino)-4-pyrimidinyl]oxy}phenyl)urea N-[4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-N'-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea N-[4-[(4-ETHYL-1-PIPERAZINYL)METHYL]-3-(TRIFLUOROMETHYL)PHENYL]-N'-[4-[[6-(METHYLAMINO)-4-PYRIMIDINYL]OXY]PHENYL]UREA Urea,N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-N'-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]- |
| CAS | 630124-46-8 |
| EINECS | 205-525-8 |
| 化学式 | C26H30F3N7O2 |
| 分子量 | 529.56 |
| 密度 | 1.341±0.06 g/cm3(Predicted) |
| 熔点 | 162-164°C |
| 沸点 | 563.1±50.0 °C(Predicted) |
| 溶解度 | DMSO (微溶) 、甲醇 (微溶) |
| 酸度系数 | 13.33±0.70(Predicted) |
| 存储条件 | under inert gas (nitrogen or Argon) at 2-8°C |
| 外观 | 固体 |
| 颜色 | White to Light Yellow |
| 体外研究 | A number of other kinases are also similarly inhibited by AST 487 (NVP-AST487) in the in vitro kinase assays, including KDR (IC 50 =170 nM), Flt-4 (IC 50 =790 nM), Flt-3 (IC 50 =520 nM), c-Kit (IC 50 =500 nM), and c-Abl (IC 50 =20 nM). AST 487 potently inhibits the growth of human thyroid cancer cell lines with activating mutations of RET but not of lines without RET mutations. Both GDNF/GFRα1 and persephin-induced calcitonin mRNA are markedly inhibited by coincubation with 100 nM of AST 487 in MTC-M cells. AST 487 is a novel, mutant FLT3 inhibitor. AST 487 is tested in biochemical assays for inhibition of Flt-3 kinase activity. The K i is determined to be 0.12 μM. Besides Flt-3, NVP-AST487 inhibits RET, KDR, c-Kit, and c-Abl kinase with IC 50 values below 1 μM. Treatment of FLT3-ITD-Ba/F3 cells and D835Y-Ba/F3 cells with AST 487 potently inhibits cellular proliferation (IC 50 <5 nM). AST 487 treatment of FLT3-ITD-Ba/F3 cells with 0.01 μM AST 487 results in complete cell killing compare with approximately 50% killing of AML patient samples at the same concentration. |
| 体内研究 | After a single oral administration of 15 mg/kg of AST 487 to OF1 mice, a mean peak plasma level (C max ) of 0.505±0.078 μM SE is achieved after 0.5 h. Similar levels of AST 487 are found in the plasma of mice up to 6 h after oral administration, with a C last of 21±4 nM at 24 h. The oral bioavailability is calculated to be 9.7% with a t 1/2 terminal elimination of 1.5 h. |
RET激酶抑制剂(AST 487) - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.888 ml | 9.442 ml | 18.884 ml |
| 5 mM | 0.378 ml | 1.888 ml | 3.777 ml |
| 10 mM | 0.189 ml | 0.944 ml | 1.888 ml |
| 5 mM | 0.038 ml | 0.189 ml | 0.378 ml |
最后更新：2024-01-02 23:10:35
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产品名: 1-(4-((4-乙基哌嗪-1-基)甲基)-3-(三氟甲基)苯基)-3-(4-((6-(甲基氨基)嘧啶-4-基)氧基)苯基)脲 去供应商网站查看 询盘CAS: 630124-46-8
产地: 北京
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规格: YS109264-10mg,YS109264-5mg
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库存: 一周左右
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产品描述: 产品覆盖：小分子化合物、分析对照品、染色试剂、生化试剂盒、细胞生物学、分子生物学、抗体、蛋白、多肽、ELISA试剂盒、微生物培养、化学合成、仪器耗材、CRO技术 更多
提供多种规格现货供应
产品名: 1-(4-((4-乙基哌嗪-1-基)甲基)-3-(三氟甲基)苯基)-3-(4-((6-(甲基氨基)嘧啶-4-基)氧基)苯基)脲 去供应商网站查看 询盘CAS: 630124-46-8
产地: 北京
包装: 瓶
规格: YS109264-10mg,YS109264-5mg
价格: 电话、微信、QQ、邮件
库存: 一周左右
电话: 010-50973130
手机: 17801761073(微信同号)
电子邮件: 3193328036@qq.com
QQ: 3193328036
微信: 17801761073
产品描述: 产品覆盖：小分子化合物、分析对照品、染色试剂、生化试剂盒、细胞生物学、分子生物学、抗体、蛋白、多肽、ELISA试剂盒、微生物培养、化学合成、仪器耗材、CRO技术 更多
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RET激酶抑制剂(AST 487) Monooctyl Itaconate 4-吡啶羧酸乙酯 4-[((5-(1-[(4-CHLOROPHENYL)SULFONYL]-4-PIPERIDINYL)-4-[3-(TRIFLUOROMETHYL)PHENYL]-4H-1,2,4-TRIAZOL-3-YL)SULFANYL)METHYL]PHENYL METHYL ETHER 4-Bromo-1-isopentyl-3-(trifluoromethyl)pyrazole POMALIDOMIDE-PEG3-叠氮化物 3-[(4-甲氧基苯基)氨基]丙腈 1,3-Benzenedicarboxylic acid, 5-methoxy-, 1-methyl ester 阿哌沙班杂质13C-D3 (6-methyl-3-pyridazinyl)hydrazine
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