| CAS |
No.1392278-76-0 |
| 英文名称 |
iRGD |
| 别名 |
c(CRGDKGPDC） |
| 分子式 |
C35H57N13O14S2 |
| 分子量 |
948.04 |
| 溶解性 |
Soluble in Water |
| 纯度 |
≥98% |
| 外观(性状) |
Solid |
| 储存条件 |
Powder:-20℃，1 year;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 |
冷藏运输 |
| SMILES |
C1C[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N2C1)CCCCN)CC(=O)O)CCCN=C(N)N)N)C(=O)O)CC(=O)O |
| InChIKey |
YHTTWXCDIRTOQX-FQJIPJFPSA-N |
| InChI |
InChI=1S/C35H57N13O14S2/c36-8-2-1-5-18-30(57)42-14-25(50)48-10-4-7-23(48)33(60)46-21(12-27(53)54)32(59)47-22(34(61)62)16-64-63-15-17(37)28(55)44-19(6-3-9-40-35(38)39)29(56)41-13-24(49)43-20(11-26(51)52)31(58)45-18/h17-23H，1-16，36-37H2，(H，41，56)(H，42，57)(H，43，49)(H，44，55)(H，45，58)(H，46，60)(H，47，59)(H，51，52)(H，53，54)(H，61，62)(H4，38，39，40)/t17-，18-，19-，20-，21-，22-，23-/m0/s1 |
| PubChem CID |
134611625 |
| 靶点 |
Integrin |
| 通路 |
Cytoskeleton |
| 背景说明 |
是一种由 9 个氨基酸组成的环肽，先与 av integrins 结合，随后酶解产生 CRGDK/R 与 神经纤毛蛋白-1 (neuropilin-1) 相互作用，从而促进药物的组织渗透，具有靶向肿瘤、肿瘤渗透的作用。 |
| 生物活性 |
iRGD peptide is a 9-amino acid cyclic peptide， triggers tissue penetration of agents by first binding to αv-integrins， then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1， and has tumor-targeting and tumor-penetrating properties.[1-2] |
| In Vitro |
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[1]. 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[2]. |
| In Vivo |
iRGD inserted in the oncolytic adenovirus ICOVIR15K (ICOVIR15K-iRGD) enhances early adenovirus dissemination through the tumor mass and elevates the antitumor effect in mice[1]. iRGD (4 mmol/kg， i.v.) in combination with 5-FU significantly suppresses the tumor growth in nude mice bearing human gastric cancer cells[2]. |
| 动物实验 |
Mice[2]12 male BALB/c nude mice (4-week-old) are assigned to 4 groups with 3 mice in each group. Among them，two groups are subcutaneously injected into the flanks by 3 × 106 HCG27 cells， the other two groups are conducted by NCI-N87 cells. Experimental groups are intravenously injected by 5-FU (25 mg/kg) mixed with iRGD peptide (4 mmol/kg) at every three days for 4 weeks while control groups are treated by 5-FU (25 mg/kg) mixed with PBS. And tumor volume is computed every 1 week with a digital vernier caliper using the following formula: tumor volume = (length × width2)/2[2]. |
| 数据来源文献 |
[1]. Puig-Saus C， et al. iRGD tumor-penetrating peptide-modified oncolytic adenovirus shows enhanced tumor transduction， intratumoral dissemination and antitumor efficacy. Gene Ther. 2014 Aug;21(8):767-74.
[2]. Zhang L， et al. Combination of NRP1-mediated iRGD with 5-fluorouracil suppresses proliferation， migration and invasion of gastric cancer cells. Biomed Pharmacother. 2017 Sep;93:1136-1143. |
| 规格 |
1mg 2mg 5mg 10mg |
| 单位 |
瓶 |
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