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KRN 633

Catalog No.
A5760
VEGFR inhibitor,ATP-competitive
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$120.00
In stock
5mg
$90.00
In stock
10mg
$145.00
In stock
50mg
$345.00
Ship with 10-15 days
100mg
$540.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

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Background

KRN 633 is a selective inhibitor of VEGFR-1, VEGFR-2 and VEGFR-3 with IC50 value of 170 nM, 160 nM and 125 nM [1].

Vascular endothelial growth factor receptor (VEGFR) is a protein and plays an important role in tumor angiogenesis by cooperating with its ligand VEGF [1].

KRN 633 is a potent VEGFR inhibitor. When tested with HUVECs, KRN 633 inhibited the cell proliferation that mediated by VEGF with the IC50 value of 14.9 nmol/L and suppressed the capillary tube formation by ~50% at the dose of 10 nmol/L [1].

In mid-pregnant mice model, KRN633 was used at the dose of 5 mg/kg once daily from embryonic day 13.5 until the day of delivery and the effect on vascular growth was slightly delayed on postnatal day 4 (P4) and on P8 it was observed that KRN633 resulted in the decreased numbers of central arteries and veins and abnormal branching of the central arteries [2]. When tested with athymic mouse xenograft HT29 cells model, administration of KRN633 inhibited tumor growth as ~90% from the initial tumor volume rangs from 500-667 mm3, while had less effect Du145 xenograft mouse models by inhibiting tumor angiogenesis and vascular permeability [1].

References:
[1].  Nakamura, K., et al., KRN633: A selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase that suppresses tumor angiogenesis and growth. Mol Cancer Ther, 2004. 3(12): p. 1639-49.
[2].  Morita, A., et al., Treatment of mid-pregnant mice with KRN633, an inhibitor of vascular endothelial growth factor receptor tyrosine kinase, induces abnormal retinal vascular patterning in their newborn pups. Birth Defects Res B Dev Reprod Toxicol, 2014. 101(4): p. 293-9.

Chemical Properties

StorageStore at -20°C
M.Wt416.86
Cas No.286370-15-8
FormulaC20H21ClN4O4
Solubility≥13.75mg/mL in DMSO with gentle warming,insoluble in EtOH,insoluble in H2O
Chemical Name1-[2-chloro-4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-3-propylurea
SDFDownload SDF
Canonical SMILESCCCNC(=O)NC1=C(C=C(C=C1)OC2=NC=NC3=CC(=C(C=C32)OC)OC)Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description KRN 633 is an ATP-competitive inhibitor of VEGFR1, 2 and 3 with IC50 values of 170 nM, 160 nM and 125 nM,respectively.
Targets VEGFR3 VEGFR2 VEGFR1      
IC50 125 nM 160 nM 170 nM      

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