MGCD-265 analog|875337-44-3|-陌孚医药/Medlife

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MGCD-265 analog

目录号: PL01809 纯度: ≥98%

CAS No. :875337-44-3

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中文名称	MGCD-265 analog
中文别名	MGCD265 抑制剂;N-(3-氟-4-(2-(1-甲基-1H-咪唑-4-基)噻吩并[3,2-B]吡啶-7-氧基)苯基氨基硫代甲酰基)-2-苯乙酰胺;氟培龙
英文名称	MGCD-265 analog
英文别名	N-((3-Fluoro-4-((2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)carbamothioyl)-2-phenylacetamide;MGCD265;MGCD-265;N-(3-fluoro-4-(2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yloxy)phenylcarbamothioyl)-2-phenylacetamide;N-[[3-fluoro-4-[2-(1-methylimidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxyphenyl]carbamothioyl]-2-phenylacetamide;MGCD 265 analog;MGCD265,MGCD-265;MGCD 265;n-(3-fluoro-4-(2-(1-methyl-1h-imidazol-4-yl)thieno(3,2-b)pyridin-7-yloxy)phenylcarbamothioyl)-2-phenylacetamide;93M6577H9D;N-((3-Fluoro-4-((2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl);MGCD-265 analog
Cas No.	875337-44-3
分子式	C₂₆H₂₀FN₅O₂S₂
分子量	517.60
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	MGCD-265 analog 是一种高效的，具有口服活性的酪氨酸激酶 c-Met 和 VEGFR2 抑制剂，其 IC₅₀ 值分别为 29 nM 和 10 nM。MGCD-265 analog 具有显著的抗肿瘤活性。
生物活性	MGCD-265 analog is a potent and oral active inhibitor of c-Met and VEGFR2 tyrosine kinases, with IC 50 s of 29 nM and 10 nM, respectively. MGCD-265 analog has significant antitumor activity.
性状	Solid
IC50 & Target[1][2]	VEGFR2 10 nM (IC50) c-Met 29 nM (IC50
体外研究(In Vitro)	MGCD-265 analog inhibits A549 cells migration and DU145 cells scattering, with IC50s of 0.4 μM and 0.08 μM, respectively, in HGF-driven cell migration and scattering assays. MGCD-265 analog inhibits HUVEC ERK phosphorylation (IC50=0.03 μM) and HUVEC proliferation (IC50=0.006 μM) in VEGF-dependent cell-based assays. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	MGCD-265 analog (20 mg/kg; p.o.) inhibits tumor growth inhibition on various human tumor models in mice. MGCD-265 analog exhibits moderate oral bioavailability (rat 12%, dog 42%) and C max (rat 0.14, dog 0.21 uM/(mg/kg)) following oral administration (rat 5-25, dog 5 mg/kg). MGCD-265 analog exhibits reasonable terminal elimination half-lives (rat 1.2, dog 5.8 h) due to plasma clearance (rat 0.33, dog 1.1 L/(kg h)) following intravenous administration (rat 2.5, dog 0.8 mg/kg) . 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]. Claridge S, et al. Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. Bioorg Med Chem Lett. 2008 May 1;18(9):2793-8.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (193.20 mM)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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