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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 |
| Smiles | C(NC1=CC(C(F)(F)F)=C(Cl)C=C1)(=O)N2CCN(C3=C4C(SC(=C4)C5=CC=C(C=C5)N6CCN(C)CC6)=NC=N3)CC2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||
| Solubility Information | DMSO: 1 mg/mL (1.62 mM), Sonication is recommended. | ||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.62 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||
Solution Preparation Table | |||||||||||
DMSO
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