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KRN 633

Cat. No. M3269
KRN 633 Structure
Size Price Availability Quantity
5mg USD 90 In stock
10mg USD 160 In stock
50mg USD 500 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

KRN 633 is a cell-permeable, reversible, ATP-competitive VEGFR kinase inhibitor with IC50 of 170 nM, 160 nM, and 125 nM for VEGFR-1, VEGFR-2, VEGFR-3, respectively. It inhibits PDGFR-α and c-Kit at higher concentrations only (IC50 = 0.97 µM and 4.33 µM, respectively) and inactive towards 17 other kinases (IC50 ≥ 10 µM). Shown to suppress VEGF-dependent, but not FGF-dependent, cellular signaling and cell proliferation. Although not cytotoxic to cancer cells, KRN633 exhibits excellent in vivo antitumor activity due to its inhibitory effects on vessel formation and vascular permeability.

Protocol
Cell Experiment
Cell lines A549, Ls174T, DU145, HT29, LNCap and PC-3 cell lines
Preparation method Plating cancer cells in media containig 10% FBS and antibiotics, at densities known to permit exponential growth over the assay period. Culturing the cells for 24 hours before adding KRN633 (0.01 to 10 μM) or just the vehicle (0.1% DMSO in medium) and then growing for a further 96 hours. Using WST-1 reagent to measure cell viability .
Concentrations Dissolved in DMSO, final concentrations 0.01 to 10 μM
Incubation time 96 hours
Animal Experiment
Animal models A549, Ls174T, HT29, DU145, LNCap, PC-3 cells and LC-6-JCK are established in athymic mice (BALB/cA, Jcl-nu) and athymic rats (F344/N, Jcl-rnu), respectively.
Formulation Suspended in vehicle (0.5% methylcellulose solution)
Dosages 20-100 mg/kg
Administration Gavage once daily
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 416.86
Formula C20H21ClN4O4
CAS Number 286370-15-8
Purity >98%
Solubility DMSO
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: KRN 633 supplier, VEGFR/PDGFR, inhibitors

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