AST 487
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- CAS号:
- 630124-46-8
- 英文名:
- AST 487
- 英文别名:
- CS-562;AST 487;NVP-AST 487;AST487 (NVP- AST487);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;3-{4-[(4-ETHYLPIPERAZIN-1-YL)METHYL]-3-(TRIFLUOROMETHYL)PHENYL}-1-(4-{[6-(METHYLAMINO)PYRIMIDIN-4-YL]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]-
- 中文名:
- AST 487
- 中文别名:
- 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;N-[4-[(4-ETHYL-1-PIPERAZINYL)METHYL]-3-(TRIFLUOROMETHYL)PHENYL]-N'-[4-[[6-(METHYLAMINO)-4-PYRIMIDINYL]OXY]PHENYL]UREA
- CBNumber:
- CB02627342
- 分子式:
- C26H30F3N7O2
- 分子量:
- 529.56
- MOL File:
- 630124-46-8.mol
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AST 487化学性质
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熔点:
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162-164°C
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沸点:
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563.1±50.0 °C(Predicted)
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密度:
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1.341±0.06 g/cm3(Predicted)
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储存条件:
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under inert gas (nitrogen or Argon) at 2-8°C
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溶解度:
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DMSO (Slightly), Methanol (Slightly)
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酸度系数(pKa):
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13.33±0.70(Predicted)
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形态:
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Solid
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颜色:
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White to Light Yellow
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AST 487性质、用途与生产工艺
AST-487 (NVP-AST487)，一种N,N'-二苯基脲，是Flt3的竞争性抑制剂，ki值为0.12 μM。除FLT3以外，AST487还抑制RET,KDR,c-KIT 和 c-ABL 激酶，IC50值低于1 μM。
| Target | Value |
RET
()
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KDR
()
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c-Kit
()
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c-Abl
()
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FLT3
(Cell-free assay)
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0.12 μM(Ki)
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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.
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.
AST 487
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-15002 | AST 487 | | 1 mg | 360元 |
| 2024/01/25 | HY-15002 | AST 487
AST 487 | 630124-46-8 | 5mg | 900元 |
630124-46-8, AST 487 相关搜索:
- 合成有机化合物配体
- 细胞生物学试剂
- 标准品
- C26H30F3N7O2
- RET激酶抑制剂(AST 487)
- N-[4-[(4-ETHYL-1-PIPERAZINYL)METHYL]-3-(TRIFLUOROMETHYL)PHENYL]-N'-[4-[[6-(METHYLAMINO)-4-PYRIMIDINYL]OXY]PHENYL]UREA
- 化合物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
- 630124-46-8
- 3-{4-[(4-ETHYLPIPERAZIN-1-YL)METHYL]-3-(TRIFLUOROMETHYL)PHENYL}-1-(4-{[6-(METHYLAMINO)PYRIMIDIN-4-YL]OXY}PHENYL)UREA
- CS-562
- Urea,N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-N'-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]-
- N-[4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-N'-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea
- AST487 (NVP- AST487)
- 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
- NVP-AST 487
- AST 487