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KRN-633 is an effective VEGFR inhibitor. The IC50s of KRN-633(KRN633) for VEGFR1, VEGFR2, and VEGFR3 is 170, 160 and 125 nM, respectively.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $41 | In Stock | In Stock | |
| 10 mg | $64 | In Stock | In Stock | |
| 25 mg | $106 | In Stock | In Stock | |
| 50 mg | $155 | In Stock | In Stock | |
| 100 mg | $230 | - | In Stock | |
| 200 mg | $328 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $45 | In Stock | In Stock |
| Description | KRN-633 is an effective VEGFR inhibitor. The IC50s of KRN-633(KRN633) for VEGFR1, VEGFR2, and VEGFR3 is 170, 160 and 125 nM, respectively. |
| Targets&IC50 | VEGFR1:170 nM, VEGFR2:160 nM, VEGFR3:125 nM |
| In vitro | In human umbilical vein endothelial cells, KRN-633 inhibits tyrosine phosphorylation of VEGFR-1, VEGFR2, c-Kit, and PDGFR-β with IC50 of 11.7, 1.16, 8.01, 130 nM, respectively. In endothelial cells, KRN-633 inhibits the formation of the capillary tube. KRN-633 suppress the VEGF-driven proliferation of HUVECs (IC50=14.9 nM). |
| In vivo | In athymic mouse and rat xenograft models, KRN-633 was able to inhibit tumor growth in various tissue sources such as lungs, colon, and prostate. It was also observed that in the non-necrosis region of tumor grafts, the number of endothelial cells was reduced and vascular permeability decreased. In the regenerated tumors, KRN-633 can also ablate tumor growth. |
| Kinase Assay | In cell-free kinase assays,with1 μM ATP the IC50 of KRN-633 is from 0.3 nM to 10 μM. |
| Cell Research | Cancer cells, such as A549, Ls174T, HT29, DU145, LNCap, and PC-3 cells, are cultured for 24 hours, then add KRN-633 (0.01 to 10 μM)that is prepared in 0.1% DMSO in the medium growing for 96 hours. |
| Animal Research | In tumor xenografts mice model, are treated with KRN-633(10-100 mg/kg) once or twice per day. In human tumor xenografts athymic rats (BALB/cA, Jcl-nu), when the tumors reach the average size indicated (162 to 657 mm3), and are treated with KRN-633 either once or twice per day. After 14days treatment, Calculate the tumor growth inhibition. |
| Synonyms | KRN633 |
| Molecular Weight | 416.86 |
| Formula | C20H21ClN4O4 |
| Cas No. | 286370-15-8 |
| Smiles | CCCNC(=O)Nc1ccc(Oc2ncnc3cc(OC)c(OC)cc23)cc1Cl |
| Relative Density. | 1.321 g/cm3 |
| 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: 6 mg/mL (14.39 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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