Cilengitide (EMD 121974) is a potent and selective inhibitor of the integrins ανβ3 and ανβ5. Cilengitide inhibits binding of isolated ανβ3 and ανβ5 to Vitronectin with an IC50 value of 4 and 79 nM, respectively .
体外研究
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 IC50's 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 .
体内研究
Cilengitide (i.p. at 10, 50, and 250 μg three times per week) inhibits M21-L melanoma tumors growth in nude mice .
Animal Model:
Nude mice bearing M21-L melanoma tumors
Dosage:
10, 50, and 250 μg
Administration:
Dosed i.p. three times per week
Result:
Demonstrated inhibition of tumor growth with a reduction in both tumor volume (55%, 75%, and 89%, respectively) and tumor weight (23%, 38%, and 61%, respectively), when compared to controls.
分子式
C27H40N8O7
分子量
588.66
CAS号
188968-51-6
中文名称
西仑吉肽
运输条件
Room temperature in continental US; may vary elsewhere.