Cilengitide is a molecule designed and synthesized at the Technical University Munich in collaboration with Merck KGaA in Darmstadt. Cilengitide binds to the activities of the αvβ3 and αvβ5 integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis. Cilengitide (EMD 121974) could increase systemic RIT efficacy of therapy in a human breast cancer tumor model having mutant p53 and expressing bcl-2. Cilengitide is currently in clinical phase III for treatment of glioblastomas and in phase II for several other tumors.
Heliyon. 2023 Jun 29;e17841.
Cilengitide inhibits osteoclast adhesion through blocking the αvβ3-mediated FAK/Src signaling pathway
Cilengitide purchased from AbMole
| Molecular Weight | 588.66 |
| Formula | C27H40N8O7 |
| CAS Number | 188968-51-6 |
| Solubility (25°C) | DMSO: ≥ 45 mg/mL |
| Storage | -20°C, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Integrin Products |
|---|
| HSDVHK-NH2
HSDVHK-NH2 is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM). |
| LDV
LDV, a tripeptide, is a non-fluorescent analog of LDV-FITC. |
| Cyclo(RADfK)
Cyclo(RADfK) is a selective α(v)β(3) integrin ligand that has been extensively used for research, therapy, and diagnosis of neoangiogenesis. |
| Obtustatin
Obtustatin is a non-RGD disintegrin of 41 residues. |
| Integrin Binding Peptide
Integrin Binding Peptide is derived by fibronectin. |
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