KRN-633

Modify Date: 2025-08-25 06:52:14

KRN-633 Structure
KRN-633 structure
Common Name KRN-633
CAS Number 286370-15-8 Molecular Weight 416.858
Density 1.3±0.1 g/cm3 Boiling Point 545.6±50.0 °C at 760 mmHg
Molecular Formula C20H21ClN4O4 Melting Point 229 °C
MSDS Chinese USA Flash Point 283.7±30.1 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of KRN-633


KRN-633 is a potent VEGFR inhibitor with IC50s of 170, 160 and 125 nM for VEGFR1, VEGFR2 and VEGFR3, respectively.

 Names

Name 1-[2-chloro-4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-3-propylurea
Synonym More Synonyms

 KRN-633 Biological Activity

Description KRN-633 is a potent VEGFR inhibitor with IC50s of 170, 160 and 125 nM for VEGFR1, VEGFR2 and VEGFR3, respectively.
Related Catalog
Target

VEGFR1:170 nM (IC50)

VEGFR2:160 nM (IC50)

VEGFR3:125 nM (IC50)

In Vitro KRN-633 inhibits tyrosine phosphorylation of VEGFR-1, VEGFR2, c-Kit, and PDGFR-β (IC50=11.7, 1.16, 8.01, 130 nM) in human umbilical vein endothelial cells. KRN-633 also inhibits the VEGF-driven proliferation of HUVECs (IC50=14.9 nM). KRN-633 suppresses capillary tube formation of endothelial cells[1].
In Vivo KRN-633 inhibits tumor growth in several tumor xenograft models with diverse tissue origins, including lung, colon, and prostate, in athymic mice and rats. KRN-633 also causes the regression of some well-established tumors and those that have regrown after the cessation of treatment. KRN-633 is well tolerated and has no significant effects on body weight or the general health of the animals. Histologic analysis of tumor xenografts treated with KRN-633 reveals a reduction in the number of endothelial cells in non-necrotic areas and a decrease in vascular permeability[1].
Kinase Assay Cell-free kinase assays are done to obtain IC50 values against a variety of recombinant receptor and non-RTKs. KRN-633 is tested from 0.3 nM to 10 μM. All assays are done in quadruplicate with 1 μM ATP[1].
Cell Assay A549, Ls174T, HT29, DU145, LNCap, and PC-3 cells cancer cells are cultured for 24 hours before adding KRN-633 (0.01 to 10 μM) or vehicle (0.1% DMSO in medium) and then grow for a further 96 hours. Cell viability is measured using WST-1 reagent. The percentage viability is determined relative to the untreated control[1].
Animal Admin Rats: Human tumor xenografts are established in the hind flank of athymic rats (BALB/cA, Jcl-nu). Rats are randomized into groups of five at the point when the tumors reach the average size indicated (162 to 657 mm3) and are then treated with KRN-633 or vehicle, either once (qd) or twice (bid) per day, at the dosages shown. The percentage of tumor growth inhibition compared with the vehicle-treated group is calculated on the day after the last treatment (day 14)[1]. Mice: The mice are randomized into groups of five at the point when the tumors reached the average sizes: 103 to 260 mm3 or 500 to 667 mm3. They are then treated with KRN-633 or vehicle, either once (qd) or twice (bid) per day, at the dosages of 10-100 mg/kg. The percentage of tumor growth inhibition (TGI) compared with the vehicle-treated group is calculated on the day after the last treatment[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 Dec;3(12):1639-49.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 545.6±50.0 °C at 760 mmHg
Melting Point 229 °C
Molecular Formula C20H21ClN4O4
Molecular Weight 416.858
Flash Point 283.7±30.1 °C
Exact Mass 416.125122
PSA 98.09000
LogP 4.14
Appearance of Characters white to beige
Vapour Pressure 0.0±1.5 mmHg at 25°C
Index of Refraction 1.629
Storage condition ?20°C
Water Solubility DMSO: soluble3mg/mL, clear (warmed)

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Hazard Codes Xn
Risk Phrases 22
RIDADR NONH for all modes of transport

 Synthetic Route

~65%

KRN-633 Structure

KRN-633

CAS#:286370-15-8

Literature: EP1153920 A1, ;

 Synonyms

N-{2-chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl}-N'-propylurea
N-(2-chloro-4-((6,7-dimethoxy-4-quinazolinyl)oxy)phenyl)-N'-propylurea
Urea, N-[2-chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N'-propyl-
1-(2-chloro-4-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-propylurea
1-{2-chloro-4-[(6,7-dimethoxyquinazolin-4-yl)oxy]phenyl}-3-propylurea
KRN633,KRN-633,KRN 633
S1557_Selleck
1-{2-Chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl}-3-propylurea
KRN633
VEGF Receptor Tyrosine Kinase Inhibitor III,KRN633
KRN 633
KRN-633
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