3-[(4-喹啉甲基)氨基]-N-[4-(三氟甲氧基)苯基]-2-噻吩甲酰胺

更新时间：2025-08-20 06:32:07

3-[(4-喹啉甲基)氨基]-N-[4-(三氟甲氧基)苯基]-2-噻吩甲酰胺结构式	常用名	3-[(4-喹啉甲基)氨基]-N-[4-(三氟甲氧基)苯基]-2-噻吩甲酰胺	英文名	OSI-930
	CAS号	728033-96-3	分子量	443.441
	密度	1.5±0.1 g/cm3	沸点	517.4±50.0 °C at 760 mmHg
	分子式	C₂₂H₁₆F₃N₃O₂S	熔点	N/A
	MSDS	N/A	闪点	266.7±30.1 °C

用途

OSI-930是Kit,KDR和CSF-1R的抑制剂,IC50分别为80 nM,9 nM和15 nM,对Flt-1,c-Raf和Lck有接近的抑制性,但对 PDGFRα/β,Flt-3和Abl抑制性较弱。

中文名	3-[(4-喹啉甲基)氨基]-N-[4-(三氟甲氧基)苯基]-2-噻吩甲酰胺
英文名	3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide
英文别名	更多

描述	OSI-930是Kit,KDR和CSF-1R的抑制剂,IC50分别为80 nM,9 nM和15 nM,对Flt-1,c-Raf和Lck有接近的抑制性,但对 PDGFRα/β,Flt-3和Abl抑制性较弱。
相关类别	信号通路 >> 蛋白酪氨酸激酶 >> c-FMS 信号通路 >> 蛋白酪氨酸激酶 >> c-Kit 研究领域 >> 癌症
参考文献	[1]. Garton AJ, et al. OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer Res. 2006, 66(2):1015-1024. [2]. Lin HL, et al. Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug. Drug Metab Dispos. 2011, 39(2), 345-350.

描述

OSI-930是Kit,KDR和CSF-1R的抑制剂,IC50分别为80 nM,9 nM和15 nM,对Flt-1,c-Raf和Lck有接近的抑制性,但对 PDGFRα/β,Flt-3和Abl抑制性较弱。

相关类别

信号通路 >> 蛋白酪氨酸激酶 >> c-FMS

信号通路 >> 蛋白酪氨酸激酶 >> c-Kit

研究领域 >> 癌症

参考文献

[1]. Garton AJ, et al. OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer Res. 2006, 66(2):1015-1024.

[2]. Lin HL, et al. Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug. Drug Metab Dispos. 2011, 39(2), 345-350.

密度	1.5±0.1 g/cm3
沸点	517.4±50.0 °C at 760 mmHg
分子式	C₂₂H₁₆F₃N₃O₂S
分子量	443.441
闪点	266.7±30.1 °C
精确质量	443.091522
PSA	91.49000
LogP	5.10
InChIKey	FGTCROZDHDSNIO-UHFFFAOYSA-N
SMILES	O=C(Nc1ccc(OC(F)(F)F)cc1)c1sccc1NCc1ccnc2ccccc12
外观性状	淡黄色至黄色固体
蒸汽压	0.0±1.3 mmHg at 25°C
折射率	1.687
储存条件	-20℃

4-喹啉甲醛

4363-93-3

N-(4-trifluorom...

728033-97-4

3-[(4-喹啉甲基)氨基]-...

728033-96-3

文献：US2004/186124 A1, ; Page/Page column 12 ;

上游产品 2
CAS号4363-93-3 4-喹啉甲醛 CAS号728033-97-4 N-(4-trifluorom...
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External Id：SNCA-p-activity-luciferase

实验名称：Human KIT proto-oncogene receptor tyrosine kinase (Type III RTKs: PDGFR, CSFR, Kit, F...
来源：IUPHAR-DB
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External Id：1805_Human

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来源：NCGC
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External Id：s-my-keats_OCIMY7-m4-1

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来源：NCGC
靶标：N/A
External Id：s-my-MM1R-m4-1

实验名称：Human fms related tyrosine kinase 1 (Type IV RTKs: VEGF (vascular endothelial growth ...
来源：IUPHAR-DB
靶标：fms related tyrosine kinase 1 (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family) [Homo sapiens]
External Id：1812_Human

实验名称：Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
来源：NCGC
靶标：N/A
External Id：s-my-mm1s-m4-1

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