SU11274|658084-23-2|(PKI-SU11274)-陌孚医药/Medlife

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SU11274 (Synonyms: PKI-SU11274)

目录号: PL02433 纯度: ≥98%

CAS No. :658084-23-2

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中文名称	SU11274
中文别名	N-(3-氯苯基)-N-甲基-3-[[3,5-二甲基-4-[(4-甲基哌嗪-1-基)羰基-1H-吡咯-2-基]亚甲基]-2-氧代-2,3-二氢-1H-吲哚-5-磺酰胺;SU11274 抑制剂
英文名称	SU11274
英文别名	SU 11274;(3z)-n-(3-chlorophenyl)-3-({3,5-dimethyl-4-[(4-methylpiperazin-1-yl)carbonyl]-1h-pyrrol-2-yl}methylene)-n-methyl-2-oxo-2,3-dihydro-1h-indole-5-sulfonamide;(3Z)-N-(3-chlorophenyl)-3-[[3,5-dimethyl-4-(4-methylpiperazine-1-carbonyl)-1H-pyrrol-2-yl]methylidene]-N-methyl-2-oxo-1H-indole-5-sulfonamide;SU-11274;SU11274 (SU-11274, SU 11274, PKI-SU11274);Sul1274;(3Z)-N-(3-chlorophenyl)-3-((3,5-dimethyl-4-[(4-methylpiperazin-1-yl)carbonyl]-1H-pyrrol-2-yl)methylene)-N-methyl-2-oxoindoline-5-sulfonamide;Met Kinase Inhibitor;PKI-SU11274;SU11274;SU-MI-2;(Z)-N-(3-chlorophenyl)-3-((3,5-dimethyl-4-(4-methylpiperazine-1-carbonyl)-1H-pyrrol-2-yl)methylene)-N-methyl-2-oxoindoline-5-sulfonamide;(3Z)-N-(3-Chlorophenyl)-3-((3,5-dimethyl-4-((4-methylpiperazin-1-yl)carbonyl)-1H-pyrrol-2-yl)methylene)-N-methyl-2-o;(3Z)-N-(3-Chlorophenyl)-3-({3,5-dimethyl-4-[(4-methylpiperazin-1-yl)carbonyl]-1H-pyrrol-2-yl}methylene)-N-methyl-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide
Cas No.	658084-23-2
分子式	C₂₈H₃₀ClN₅O₄S
分子量	568.09
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	SU11274 是一种选择性的 Met 抑制剂，IC₅₀ 值为 10 nM，对 PGDFRβ，EGFR 或 Tie2 没有抑制作用。
生物活性	SU11274 is a selective Met inhibitor with IC 50 of 10 nM, but has no effects on PGDFRβ, EGFR or Tie2.
性状	Solid
IC50 & Target[1][2]	IC50: 10 nM (Met)
体外研究(In Vitro)	SU11274 exhibits greater than 50-fold selectivity for Met versus Flk and more than 500 times selectivity versus other tyrosine kinases such as FGFR-1, c-src, PDGFbR, and EGFR. SU11274 inhibits the phosphorylation of key regulators of the PI3K pathway, including AKT, FKHR, or GSK3β. SU11274 treatment inhibits the growth of TPR-MET-transformed BaF3 cells in a dose-dependent manner with IC50 of < 3 μM in the absence of interleukin 3, without growth inhibition of BaF3 cells transformed by other oncogenic tyrosine kinases, including BCR-ABL, TEL-JAK2, TEL-ABL, and TEL-PDGFβR. In addition to cell growth, SU11274 treatment significantly inhibits the migration of BaF3. TPR-MET cells by 44.8% and 80% at 1 μM and 5 μM, respectively. SU11274 inhibits HGF-dependent phosphorylation of Met as well as HGF-dependent cell proliferation and motility with an IC50 of 1-1.
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]. Wang X, et al. Potent and selective inhibitors of the Met [hepatocyte growth factor/scatter factor (HGF/SF) receptor] tyrosine kinase block HGF/SF-induced tumor cell growth and invasion. Mol Cancer Ther, 2003, 2(11):1085-1092. [2]. Sattler M, et al. A novel small molecule met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase. Cancer Res, 2003, 63(17), 5462-5469.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (176.03 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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