- Cyclo (-RGDfK)
- BIO 1211
- BIO 5192
CilengitideIntegrin inhibitor for αvβ3 and αvβ5 |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.11%
- COA (Certificate Of Analysis)
- HPLC(Retest)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
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Chemical structure
Related Biological Data
Description | Cilengitide is a small-molecule inhibitor of integrins with IC50 values of 2.3 nM and 37 nM for αvβ3 and αvβ5, respectively. | |||||
Targets | αvβ3 | αvβ5 | α5β1 | |||
IC50 | 2.3 nM | 37 nM |
Cell experiment [1]: | |
Cell lines | meningioma lines (Ben-Men1, IOMM-Lee, HBL-52) |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
Reaction Conditions | 24 h; 100 μM/mL |
Applications | Cilengitide(1, 10, and 100 μM/mL) was added to IOMM-Lee,HBL52, and Ben-Men1 cultures. Morphologic changes were monitored over 24 hours. In all three meningioma lines, cells strated to round up and detach from the flask in a concentration-dependent manner, showing that cilengitide decreases cell adhesion. Quantification of cell viability after 24 hours, cilengitide treatment showed in all three cell lines a highly significant dose-dependent but rather mild decline of viable cells. |
Animal experiment [1]: | |
Animal models | 8- to 10-week-old Swiss Nude mice |
Dosage form | 75 mg/kg; intraperitoneal injection |
Applications | We intended to test a daily dosage of cilengitide (75 mg/kg) as a monotherapy or combined with irradiation in the orthotopic mouse model. A significant reduction of tongue-like brain invasion (P≤0.01) could be observed in tumors of mice treated with either cilengitide alone (35% decrease) or with cilengitide and irradiation (35.5% decrease). |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Wilisch-Neumann A, Kliese N, Pachow D, et al. The integrin inhibitor cilengitide affects meningioma cell motility and invasion[J]. Clinical Cancer Research, 2013, 19(19): 5402-5412. |
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Cas No. | 188968-51-6 | SDF | Download SDF |
Synonyms | N/A | ||
Chemical Name | 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 | ||
Canonical SMILES | CC(C)C1C(=O)NC(C(=O)NCC(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)CC(=O)O)CCCN=C(N)N | ||
Formula | C27H40N8O7 | M.Wt | 588.66 |
Solubility | ≥29.433mg/mL in DMSO | Storage | Store at -20°C |
Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
Cilengitide is a cyclic RGD pentapeptide [Arg-Gly-Asp-DPhe-(NMeVal)], and a potent αvβ3 and αvβ5 integrin inhibitor to block integrin-mediated adhesion and migration. It can directly bind αvβ3 integrin. Its IC50 is 250 nM as an αvβ3 inhibitor [1] [2] [3] [4].Integrins are named for a family including 24 transmembrane heterodimer receptors that are composed of paired alpha and beta chains. These receptors can integrate extracellular and intracellular activities. Consequently, they can regulate tumor angiogenesis, migration and invasion [2].When treated with cilengitide, a significant dose-dependent reduction of proliferation was noted (p<0.0002) in cell lines developed through 28 d of expansion and hence 14 d of differentiation culture of CD133+ stem cells (with VEGF, SCGF and FLT3L, to prepare CD133+ EPCs, i.e. endothelial progenitor cells). When treated with cilengitide after withdrawal of FLT3L and SCGF, a dose-dependent decrease of adherent cells was noted in EPCs after 7 and 14 days (p<0.03). Compared with which on EPC proliferation, the inhibitory effect of cilengitide on endothelial cell attachment was more pronounced [3].Therapy with cilengitide intraperitoneally 5 times per week between days 1 and 30 after injection of MDA-MB-231 cells (105), volumes of osteolytic lesions(OL) and soft tissue components(SC) were significantly reduced on days 30 and 35 in rats, compared with untreated nude rats (p<0.05) [5].References: [1]. Carlos Mas-Moruno, Florian Rechenmacher and Horst Kessler. Cilengitide: The First Anti-Angiogenic Small Molecule Drug Candidate. Design, Synthesis and Clinical Evaluation. Anti-Cancer Agents in Medicinal Chemistry, 2010, 10(10): 753-768.[2]. David A Reardon, L Burt Nabors, Roger Stupp, et al. Cilengitide: an integrin-targeting arginine-glycine-aspartic acid peptide with promising activity for glioblastoma multiforme. Expert Opin Investig Drugs, 2008, 17(8):1225-1235.[3]. Sonja Loges, Martin Butzal, Jasmin Otten, et al. Cilengitide inhibits proliferation and differentiation of human endothelial progenitor cells in vitro. Biochemical and Biophysical Research Communications, 2007, 357: 1016-1020.[4]. Despoina Sykoutri, Nisha Geetha, Silvia Hayer, et al. αvβ3 Integrin Inhibition with Cilengitide both Prevents and Treats Collagen Induced Arthritis. Ann Rheum Dis, 2013, 72(Suppl 1):A1-A88.[5]. Maren Bretschi, Maximilian Merz, Dorde Komljenovic, et al. Cilengitide inhibits metastatic bone colonization in a nude rat model. Oncology Reports, 2011, 26:843-851.
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《血管紧张素转换酶抑制剂在心血管病中应用的中国专家共识》.PDF(242.69k)
1、测定酶比活力:底物需要过量么?测定时间多长?是否可以加入过量的底物,然后测定3min吸光度的增加值,从吸光度的变化值计算比活力。
2、在酶抑制剂筛选的过程中,是否需要保证底物过量?还是要水浴一定时间让反应完全?我看到文献说用终浓度为0.1μmol/mL的底物,终浓度为45U/ml的酶,我想问,假设总体积为1ml,那么终浓度为45U/ml的酶岂不是每分钟能转化4.8μmol的底物?那么0.1μmol/mL的底物不就几秒钟就反应完了?那么怎么测定初速度?
1.对于抑制剂筛选工作(求ic50)是不是体系内酶与底物的量(底物应该是过量的)对实验结果影响不大。
2.如果要求算Km值,是不是需要知道反应产物的绝对量。反应时间文献上都是5分钟,反应速度就用反应产物量除以反应时间即可。
3.酶是进口分装的,规格5U,一次用不完,用PBS稀释后如何保存
谢谢
2、可逆抑制剂:包括
a、竞争性抑制剂,抑制剂与底物竞争性结合酶反应中心,使Km增大,而Vmax不变 b、非竞争性抑制剂,酶与抑制剂结合后还能与底物结合,但活性降低,使Vmax减小,而Km不变
c、反竞争性抑制剂,酶只能与底物结合后才能与抑制剂结合,Vmax与Km都减小
可逆抑制剂可用透析等方法除去,使酶恢复作用
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