Cilengitide|188968-51-6|(西仑吉肽; EMD 121974)-陌孚医药/Medlife

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Cilengitide (Synonyms: 西仑吉肽; EMD 121974)

目录号: PL08972 纯度: ≥99%

CAS No. :188968-51-6

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中文名称	Cilengitide
中文别名	西仑吉肽;环(L-精氨酰甘氨酰-L-天冬氨酰-D-苯丙氨酰-N-甲基-L-缬氨酰);倍他司汀二盐酸盐
英文名称	Cilengitide
英文别名	Cilengitide;Cyclo(L-arginylglycyl-L-aspartyl-D-phenylalanyl-N-methyl-L-valyl);2-[(2S,5R,8S,11S)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-7-methyl-3,6,9,12,15-pentaoxo-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid;C27H40N8O7;Cilengitide [USAN:INN];cyclo(arginyl-glycyl-aspartyl-D-phenylalanyl-N-methyl-valyl);cyclo(L-arginylglycyl-L-a-aspartyl-D-phenylalanyl-N-methyl-L-valyl);Cyclo(L-arginylglycyl-L-α-aspartyl-D-phenylalanyl-N-methyl-L-valyl);cyclo(RGDf-N(Me)V-);cyclo[-Arg-Gly-Asp-D-Phe-N-MeVal-];EMD 121974;EMD-121974;NSC 707544;c(RGDf(NMe)V);Cyclo(Arg-Gly-Asp-D-Phe-N-Me-Val);Cilengitide(EMD121974,NSC-707544);2-((2S,5R,8S,11S)-5-Benzyl-11-(3-guanidinopropyl)-8-isopropyl-7-methyl-3,6,9,12,15-pentaoxo-1;Cilengitide, >=98%;EMD121974;4EDF46E4GI;Cyclo(L-arginylglycyl-L-alpha-aspartyl-D-phenylalanyl-N-methyl-L-valyl);2-((2
Cas No.	188968-51-6
分子式	C₂₇H₄₀N₈O₇
分子量	588.66
包装储存	Powder -20°C 3 years；In solvent -80°C 6 months

产品详情

Cilengitide (EMD 121974) 是一种强效的整合素拮抗剂，IC₅₀ 分别为 0.61 nM (α_νβ₃)，8.4 nM (α_νβ₅) 和 14.9 nM (α₅β₁)。Cilengitide 抑制 α_νβ₃ 和 α_νβ₅ 与玻连蛋白结合，IC₅₀ 值分别为 4 和 79 nM。Cilengitide 能够抑制 TGF-β/Smad 信号通路，调节 PD-L1 表达。Cilengitide 诱导凋亡 (apoptosis)，在对胶质母细胞瘤和其他癌症的研究中也显示出抗血管生成的作用。

生物活性

Cilengitide (EMD 121974) is a potent integrins antagonist with IC 50 s of 0.61 nM (α ν β 3 ), 8.4 nM (α ν β 5 ) and 14.9 nM (α 5 β 1 ), respectively. Cilengitide inhibits the binding of α ν β 3 and α ν β 5 to Vitronectin with IC 50 s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers.

性状

Solid

IC50 & Target[1][2]

αvβ3 4 nM (IC50, αvβ3-Vitronectin interaction) αvβ5

体外研究(In Vitro)

Cilengitide is a cyclized RGD (Arg-Gly-Asp motif)-containing pentapeptide. Cilengitide blocks integrin ανβ3- and ανβ5-mediated endothelial cell attachment and migration.
Cilengitide inhibits integrin-mediated binding to Vitronectin with IC50s of 0.4 and 0.4 μM in cell adhesion studies assessing the human melanoma M21 or UCLA-P3 human lung carcinoma cell lines.
Cilengitide inhibits the attachment of human umbilical vein endothelial cells to Vitronectin with an IC50 of 2 μM.
Cilengitide (0-1 mg/mL; 24-72 h) inhibits cell viability of melanoma cells in vitro and (5 μg/mL; 12 h) induces B16 and A375 cells apoptosis.
Cilengitide (5 μg/mL, 10 μg/mL; 2 weeks) inhibits colony formation of B16 and A375 cells.
Cilengitide (0-20 μg/mL; 12 h) inhibits STAT3 phosphorylation to decrease the expression of PD-L1.

体内研究(In Vivo)

Cilengitide (i.p. at 10, 50, and 250 μg three times per week) inhibits M21-L melanoma tumors growth in nude mice.
Cilengitide (50 mg/kg; i.p.; daily) enhances the function of CD8+ T cells and promotes anti-PD1 efficacy with Anti-PD1 monoclonal antibody in B16 murine melanoma model.
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；In solvent -80°C 6 months

ClinicalTrial

参考文献

[1]. Kapp TG, et al. A Comprehensive Evaluation of the Activity and Selectivity Profile of Ligands for RGD-binding Integrins. Sci Rep. 2017 Jan 11;7:39805.
[2]. Hariharan S, et al. Assessment of the biological and pharmacological effects of the alpha nu beta3 and alpha nu beta5 integrinreceptor antagonist, Cilengitide (EMD 121974), in patients with advanced solid tumors. Ann Oncol. 2007 Aug;18(8):1400-7.

溶解度数据	In Vitro: H₂O : 100 mg/mL (169.88 mM; Need ultrasonic)DMSO : ≥ 44 mg/mL (74.75 mM)

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Data Sheet

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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