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Cat. No. Name Size Price Add Cart
KI3335KRN 633QuoteQuote

Chemical Characteristic

Product NameKRN 633
CAS No.286370-15-8
Molecular Weight 416.86
FormulaC20H21ClN4O4
Chemical Name1-[2-chloro-4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-3-propylurea
SmilesN(C(=O)NCCC)c1c(cc(cc1)Oc1ncnc2c1cc(c(c2)OC)OC)Cl
Chemical Structure

Biological activities

KRN 633 is a novel quinazoline urea derivative and a potent ATP-competitive inhibitor of VEGFR-1, -2 and -3 with IC50s of 170, 160, and 125 nM, respectively. KRN 633 also weakly inhibits PDGF receptor (PDGFR)-α and -β, c-Kit, breast tumor kinase, and tunica interna endothelial cell kinase tyrosine kinases with IC50s of 0.97, 9.85, 4.33, 9.20, and 9.90 µM, respectively. KRN 633 also blocks the activation of mitogen-activated protein kinases (MAPK) by VEGF. In vitro, KRN 633 inhibits tyrosine phosphorylation of VEGFR-2 with an IC50 of 1.16 nM in human umbilical vein endothelial cells (HUVECs). Using a [3H]thymidine incorporation assay in vitro, KRN 633 inhibits the VEGF-driven proliferation of HUVECs with an IC50 of 14.9 nM.[1] Furthermore, KRN 633 also suppresses HIF-1α expression by inhibiting both Akt and ERK phosphorylation signaling pathways.[2] In athymic mice and rats in vivo, KRN 633 treatment potently inhibits tumor growth in several tumor xenograft models with diverse tissue origins, including lung, colon, and prostate. In athymic rats bearing A549 tumors, KRN 633 treatment at dose of 2, 10, and 50 mg/kg (twice daily p.o. for 14 days) decreases the numbers of CD31+ cells in viable regions of the tissue by 15%, 53%, and 76%, respectively.[1] Using pregnant mice in vivo, p.o. administration of KRN 633 (300 mg/kg) inhibits vascular development of placenta and fetus without obvious health impairments of mother mice, and increases the risk of induction of intrauterine growth restriction.[3]

Protocols

In vitro: Prior to use, KRN 633 is dissolved in DMSO.[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): 1639-1649.
[2] Ban HS, et al. Suppression of hypoxia-induced HIF-1alpha accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633. Cancer Lett. 2010, 296(1): 17-26.
[3] Wada Y, et al. Effects of KRN633, an inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase, on vascular development of placenta and fetus of mid-pregnancy in mice. J Pharmacol Sci. 2010, 112(3): 290-298.

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