AST 487,英文名:AST 487,CAS:630124-46-8,化学式:C26H30F3N7O2,分子量:529.56,密度:1.341±0.06 g/cm3(Predicted),熔点:16_信息_文库

AST 487,英文名:AST 487,CAS:630124-46-8,化学式:C26H30F3N7O2,分子量:529.56,密度:1.341±0.06 g/cm3(Predicted),熔点:16

2024-11-07 0

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630124-46-8 询问AST 487(AST 487)CAS: 630124-46-8化学式: C26H30F3N7O2function qrload() {var head = document.getElementsBy

630124-46-8

AST 487(AST 487)

CAS: 630124-46-8

化学式: C26H30F3N7O2

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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.

630124-46-8 - 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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