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1392278-76-0

中文名稱 1392278-76-0
英文名稱 iRGD
CAS 1392278-76-0
分子式 C35H57N13O14S2
分子量 948.04
MOL 文件 1392278-76-0.mol
更新日期 2024/12/26 08:59:53
1392278-76-0 結(jié)構(gòu)式 1392278-76-0 結(jié)構(gòu)式

基本信息

中文別名
化合物IRGD PEPTIDE
腫瘤多肽H-CYS-ARG-GLY-ASP-LYS-GLY-PRO-ASP-CYS-OH
H-CYS-CYS-ARG-GLY-ASP-LYS-GLY-PRO-ASP-CYS-OH(DISULFIDE BRIDGE:CYS2-CYS10)
英文別名
iRGD
iRGD TFA
c(CRGDKGPDC)
L-Cysteine, L-cysteinyl-L-arginylglycyl-L-α-aspartyl-L-lysylglycyl-L-prolyl-L-α-aspartyl-, cyclic (1→9)-disulfide

物理化學(xué)性質(zhì)

密度1.68±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C, protect from light
酸度系數(shù)(pKa)2.92±0.70(Predicted)
形態(tài)Solid
顏色White to off-white
水溶解性Water : ≥ 50 mg/mL (52.74 mM)
序列H-Cys-Arg-Gly-Asp-Lys-Gly-Pro-Asp-Cys-OH(Disulfide bridge: Cys1-Cys9)

常見問題列表

生物活性
iRGD peptide 是一種由 9 個(gè)氨基酸組成的環(huán)肽,先與 av integrins 結(jié)合,隨后酶解產(chǎn)生 CRGDK/R 與 神經(jīng)纖毛蛋白-1 (neuropilin-1) 相互作用,從而促進(jìn)藥物的組織滲透,具有靶向腫瘤、腫瘤滲透的作用。
靶點(diǎn)

Integrin

體外研究

iRGD peptide-mediated tumor penetration occurs in three steps: binding to αv-integrins on tumor vasculature or tumor cells, exposure by proteolysis of a C-terminal motif that binds to neuropilin-1 (NRP-1) and cell internalization. iRGD peptide inserted in the ICOVIR15K fiber C terminus enhances binding and internalization only in MCF7 cells, which express NRP-1 and integrins. iRGD insertion does not impair virus infection and replication. iRGD peptide alone has no obvious effect on gastric cancer cells, and when combined with 5-FU, iRGD peptide (0.3 μmol/mL) enhances the chemotherapy efficacy of 5-FU on gastric cancer cells through NRP1.

體內(nèi)研究

iRGD inserted in the oncolytic adenovirus ICOVIR15K (ICOVIR15K-iRGD) enhances early adenovirus dissemination through the tumor mass and elevates the antitumor effect in mice. iRGD (4 mmol/kg, i.v.) in combination with 5-FU significantly suppresses the tumor growth in nude mice bearing human gastric cancer cells.

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