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VEGFR-3-IN-1 is a novel, potent, and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. It exhibits antitumor activity, inactivates the VEGFR3 signaling pathway, and inhibits the proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $48 | In Stock | |
5 mg | $113 | In Stock | |
10 mg | $189 | In Stock | |
25 mg | $378 | In Stock | |
50 mg | $619 | In Stock | |
100 mg | $993 | In Stock | |
500 mg | $1,980 | In Stock |
Description | VEGFR-3-IN-1 is a novel, potent, and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. It exhibits antitumor activity, inactivates the VEGFR3 signaling pathway, and inhibits the proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells. |
Targets&IC50 | VEGFR3:110.4 nM |
In vitro | VEGFR-3-IN-1 (50, 25 mg/kg; oral; once; nude mice) achieved the most potent tumor volume inhibition in nude mice, with an inhibition rate of 61.9%.The results of VEGFR-3-IN-1 (10 mg/kg; oral) post-treatment showed a maximal concentration (Cmax) of 420 ng/mL, an AUC0-t of 9219 ng-h /mL, AUC0-∞ of 12,304 ng-h/mL, and a half-life (t1/2) of 16 hours. |
In vivo | VEGFR-3-IN-1 (50, 25 mg/kg; oral; once; nude mice) achieved the most potent tumor volume inhibition in nude mice, with an inhibition rate of 61.9%.The results of VEGFR-3-IN-1 (10 mg/kg; oral) post-treatment showed a maximal concentration (Cmax) of 420 ng/mL, an AUC0-t of 9219 ng-h /mL, AUC0-∞ of 12,304 ng-h/mL, and a half-life (t1/2) of 16 hours. |
Molecular Weight | 616.1 |
Formula | C29H29ClF3N7OS |
Cas No. | 2756668-73-0 |
Storage | Shipping with blue ice. |
Solubility Information | DMSO: 1 mg/ml, Sonication is recommended. |
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