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KRN-633

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Catalog No. T6137Cas No. 286370-15-8
Alias KRN633

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.

KRN-633

KRN-633

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Purity: 99.73%
Catalog No. T6137Alias KRN633Cas No. 286370-15-8
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$41In StockIn Stock
10 mg$64In StockIn Stock
25 mg$106In StockIn Stock
50 mg$155In StockIn Stock
100 mg$230-In Stock
200 mg$328-In Stock
1 mL x 10 mM (in DMSO)$45In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.73%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
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.
SynonymsKRN633
Chemical Properties
Molecular Weight416.86
FormulaC20H21ClN4O4
Cas No.286370-15-8
SmilesCCCNC(=O)Nc1ccc(Oc2ncnc3cc(OC)c(OC)cc23)cc1Cl
Relative Density.1.321 g/cm3
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.3989 mL11.9944 mL23.9889 mL119.9443 mL
5 mM0.4798 mL2.3989 mL4.7978 mL23.9889 mL
10 mM0.2399 mL1.1994 mL2.3989 mL11.9944 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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