KRN-633

SKU: orb1301043

Description

KRN-633 is a potent small molecule inhibitor targeting vascular endothelial growth factor receptors (VEGFRs), with IC50 values of 170 nM for VEGFR1, 160 nM for VEGFR2, and 125 nM for VEGFR3. It is widely used in preclinical research to study angiogenesis and tumor growth in both cellular assays and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 286370-15-8
• MW: 416.86
• Purity: 99.73% (May vary between batches)
• Formula: C₂₀H₂₁ClN₄O₄
• SMILES: CCCNC(=O)Nc1ccc(Oc2ncnc3cc(OC)c(OC)cc23)cc1Cl
• Target: VEGFR
• Solubility: DMSO:6 mg/mL (14.39 mM)

Bioactivity

• Target IC50:
  VEGFR1:170 nM|VEGFR2:160 nM|VEGFR3:125 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.
• 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).
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, KRN 633, KRN633, KRN-633, inhibit, VEGFR1, VEGFR, VEGFR3, VEGFR2, Vascular endothelial growth factor receptor

Compound Identifiers

PubChem CID

9549295