SYN1143|913376-84-8|-陌孚医药/Medlife

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SYN1143

目录号: PL04798 纯度: ≥99%

CAS No. :913376-84-8

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中文名称	SYN1143
中文别名	N-[3-氟-4-[(7-甲氧基喹啉-4-基)氧基]苯基]-1-(2-羟基-2-甲基丙基)-5-甲基-3-氧代-2-苯基-2,3-二氢-1H-吡唑-4-甲酰胺
英文名称	SYN1143
英文别名	AMG-1;N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide;N-[3-fluoro-4-[(7-methoxy-4-quinolinyl)oxy]phenyl]-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenyl-4-pyrazolecarboxamide;N-(3-Fluoro-4-((7-methoxyquinolin-4-yl)oxy)phenyl)-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide;Substituted Pyrazolone, 7;BDBM24465;C31H29FN4O5;CHE;N-[3-Fluoro-4-(7-methoxyquinolin-4-yl)oxyphenyl]-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-pheny;SYN1143;N-[3-Fluoro-4-[(7-methoxy-4-quinolinyl)oxy]phenyl]-2,3-dihydro-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenyl-1H-pyrazole-4-carboxamide (ACI);Kin001-237;Kin237;N-[3-Fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl]-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide;SYN 1143
Cas No.	913376-84-8
分子式	C₃₁H₂₉FN₄O₅
分子量	556.58
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	SYN1143 是一种有效，选择性和具有口服活性的 c-Met/RON 的双重抑制剂，IC₅₀ 值分别为 4 和 9 nM。SYN1143 对 Lck，Tie2，Src 和 BTK 的抑制活性较弱，IC₅₀ 值为 160 至 710 nM。SYN1143 可用于癌症的研究。
生物活性	SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC 50 s of 4 and 9 nM, respectively. SYN1143 has weak inhibitory activity on Lck, Tie2, Src, and BTK with IC 50 s ranging from 160 to 710 nM. SYN1143 can be used for the research of cancers that RON and c-Met are activated.
性状	Solid
IC50 & Target[1][2]	RON 9 nM (IC50)
体外研究(In Vitro)	SYN1143 (Compound I) (10-1000 nM; 1 h) inhibits c-Met-mediated signaling and functional activity in HT-29 and BxPC3 cells. SYN1143 (10-1000 nM; 1 h) inhibits RON-mediated signaling and functional activity in NIH3T3 RON and BxPC3 cells. SYN1143 (0.3-30 μM; 2 h or 3 d) inhibits c-Met signaling and cell proliferation in MC3T3-E1 and C3H10T1/2 cells. SYN1143 (0.3-2 μM; 4-12 d) potentiates osteogenic differentiation of precursor cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	SYN1143 (10-100 mg/kg; p.o. for 22 d) inhibits the growth of c-Met-dependent and constitutively active RON-expressing tumors in mice. SYN1143 (20-50 μg; transferred into calvarial defects) stimulates bone formation in critical-sized defects of mouse calvarial bone. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Zhang Y, et, al. Identification of a novel recepteur dorigine nantais/c-met small-molecule kinase inhibitor with antitumor activity in vivo. Cancer Res. 2008 Aug 15;68(16):6680-7. [2]. Kim JW, et, al. Chemical inhibitors of c-Met receptor tyrosine kinase stimulate osteoblast differentiation and bone regeneration. Eur J Pharmacol. 2017 Jul 5;806:10-17.

溶解度数据	In Vitro: DMSO : 100 mg/mL (179.67 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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