Detail introduction: Cilengitide/188968-51-6
| English name | cilengitide |
| CAS NO | 188968-51-6 |
| Peptide sequence | Cyclo(Arg-Gly-Asp-Dphe-NMeVal) |
| Molecular formula | C27H40N8O7 |
| Molecular weight | 588.66 |
| storage temperature | 2-8℃ |
| purity | ≥98% |
| Package | 1mg;5mg;10mg;50mg;100mg,1g or according to customer’s detail requirement. |
| Product English synonyms | EMD 121974;CS-1500;CS-2674 |
What is Cilengitide?
Cilengitide is a potent and selective αvβ3 and αvβ5 receptor integrin inhibitor with IC50 of 4 and 79 nM, respectively.
In vitro study of EMD 121974
EMD 121974 is a αvβ3 and αvβ5 integrin receptor antagonist. In evaluating cell adhesion studies of human melanoma M21 or UCLA-P3 human lung cancer cell lines
It inhibited integrin-mediated binding to vitronectin with IC50 of 0.4 and 0.4 μM, respectively.
The in vitro therapeutic concentration of it is greater than 1 μM, showing a concentration and time-dependent cytotoxicity.
However, lower doses of cilengitide monotherapy (0.1 and 0.5μM) did not cause effective death of U87MG and U251MG cells.
Significant cytotoxicity was observed in U87MG cells, in which 1 μM was added in combination with Belotecan monotherapy at a concentration of 6.25 nM. Compared with lower concentrations of EMD 121974 (1μM), higher concentrations of EMD 121974(5 and 25μM) did not significantly increase cell death in U87MG and U251MG.
Cilengitide in vivo study
In nude mice carrying M21-L melanoma, It was injected intraperitoneally at doses of 10, 50 and 250 μg three times a week, which showed inhibition of tumor growth and reduced tumor volume (respectively 55%, 75% and 89%) )
Compared with the control group, the tumor weight (23%, 38% and 61% respectively).
In the rat model studied, the systemic pharmacokinetics of ip It was not affected by the ILP of cilengitide alone or the ILP of cilengitide plus melphalan, TNF or both.
Within 10 minutes of administration, the systemic It level reached about 20μg/mL (about 35μM), and continued to rise to about 40μg/mL (about 70μM) within the first hour.
After that, the level of cilengitide in the serum decreased, and the elimination half-life was 2.1 hours.
Where to buy cilengitide in the US
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