E7820 is a α2 integrin inhibitor which suppressing integrin alpha 2, a cell adhesion molecule expressed on endothelial cells. E7820 inhibits proliferation of HUVEC induced by either bFGF and VEGF in serum-free medium with IC50 values of 0.10 and 0.081 μg/mL, respectively.
In vivo, E7820 (50 mg/kg) with erlotinib has a significantly synergistic antitumor effect in three xenograft models. E7820 (50, 100, and 200 mg/kg) inhibits tumor growth in a dose-dependent manner in all s.c. xenograft models. E7820 completely inhibits s.c. tumor growth of LoVo tumor cells and also regresses the tumor mass of KP-1 tumor cells at the dosages of both 100 and 200 mg/kg.
Molecular Weight | 336.37 |
Formula | C17H12N4O2S |
CAS Number | 289483-69-8 |
Solubility (25°C) | DMSO ≥ 70 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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 |
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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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