| 名稱 | MGCD-265 analog |
| 描述 | MGCD-265 analog (Glesatinib) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nM and 10 nM for c-Met and VEGFR2, respectively. |
| 細(xì)胞實(shí)驗(yàn) | Cells are treated with MGCD-265 for 72 hours and cell number is determined as a function of mitochondrial activity, following incubation with MTT for 4 hours.(Only for Reference) |
| 激酶實(shí)驗(yàn) | Time-resolved fluorescence resonance energy transfer assay: The c-Met–catalyzed phosphorylation of N-biotinylated peptide (EQEDEPEGDYFEWLE-CONH2) is measured using a time-resolved fluorescence resonance energy transfer assay. [2] The MK-2461 IC50 for Ron, Mer, Flt1, Flt3, Flt4, KDR, PDGFRβ, FGFR1, FGFR2, FGFR3, TrkA, and TrkB are determined using time-resolved fluorescence resonance energy transfer assays similar to the c-Met kinase assay. |
| 體外活性 | MGCD-265是一種多靶點(diǎn)受體酪氨酸激酶抑制劑，對Met, MetY1235D, MetM1250T, VEGFR1, VEGF2, VEGF3, Ron和Tie2顯示出強(qiáng)效抑制作用，IC50值在1 nM至7 nM范圍。[1] MGCD-265在c-Met驅(qū)動(dòng)的腫瘤細(xì)胞（MKN45, MNNG-HOS, SNU-5）和非c-Met驅(qū)動(dòng)的腫瘤細(xì)胞（HCT116和MDA-MB-231）中均能抑制細(xì)胞增殖，IC50值分別為6 nM–30 nM和1 μM–3 μM。在血清饑餓的MKN45細(xì)胞中，MGCD-265（40 nM–5 μM）有效抑制c-Met磷酸化及其下游信號通路，包括Erk, Akt, Stat3和Fak。MGCD-265（6 nM–1 μM）還能誘導(dǎo)MKN45細(xì)胞發(fā)生凋亡。 |
| 體內(nèi)活性 | 在c-Met驅(qū)動(dòng)或非c-Met驅(qū)動(dòng)的MKN45、U87 mg、MDA-MB-231、COLO205和A549腫瘤細(xì)胞小鼠異種移植模型中，MGCD-265（20 mg/kg–60 mg/kg）抑制腫瘤生長和c-Met信號傳導(dǎo)。MGCD-265（40 mg/kg）還在帶有U87 mg異種移植物的小鼠的腫瘤和血漿中下調(diào)與血管生成相關(guān)的基因表達(dá)，包括VEGF和IL-8。MGCD-265也抑制了shed-Met在血漿中的水平。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 96 mg/mL (185.5 mM)
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| 關(guān)鍵字 | VEGFR | cell | angiogenesis | kinases | MGCD265 | proliferation | MGCD-265 analog | Inhibitor | MGCD 265 | morphogenesis | c-Met/HGFR | Apoptosis | invasion | MGCD265 analog | Vascular endothelial growth factor receptor | inhibit | survival | MGCD 265 analog | migration | receptor | tyrosine |
| 相關(guān)產(chǎn)品 | L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate |
| 相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 抗癌活性化合物庫 | 已知活性化合物庫 | 激酶抑制劑庫 | 膜蛋白靶向化合物庫 | 酪氨酸激酶分子庫 | 藥物功能重定位化合物庫 | 抗癌臨床化合物庫 | 抗癌藥物庫 |