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KRN-633

Chemical Structure : KRN-633

CAS No.: 286370-15-8

KRN-633 (KRN 633;KRN633)

Catalog No.: PC-42875Not For Human Use, Lab Use Only.

KRN-633 is a potent, selective VEGFR-2 inhibitor that inhibist the phosphorylation of VEGFR-2 with IC50 of 1.16 nM, also inhibits VEGFR-1, c-Kit and PDGFR-β with IC50 of 11.7, 8.01 and 130 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

KRN-633 is a potent, selective VEGFR-2 inhibitor that inhibist the phosphorylation of VEGFR-2 with IC50 of 1.16 nM, also inhibits VEGFR-1, c-Kit and PDGFR-β with IC50 of 11.7, 8.01 and 130 nM; does not inhibits the phosphorylation of FGFR-1, EGFR, or c-Met at 10 uM; blocks the activation of mitogen-activated protein kinases by VEGF, inhibits VEGF-driven proliferation of HUVECs with IC50 of 14.9 nM; inhibits tumor growth in several in vivo tumor xenograft models with diverse tissue origins, including lung, colon, and prostate, in athymic mice and rats.

Solid Tumors

Phase 1 Clinical

Physicochemical Properties

M.Wt 416.8582
Formula C20H21ClN4O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Urea, N-[2-chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N'-propyl-

References

1. Matsunaga N, et al. Mol Cancer Ther. 2006 Jan;5(1):80-8.

2. Wada Y, et al. J Pharmacol Sci. 2010;112(3):290-8.

3. Morita A, et al. Exp Eye Res. 2014 Mar;120:127-37.

4. Nakamura K, et al. Mol Cancer Ther. 2004 Dec;3(12):1639-49.

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