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KRN 633

KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 170 nM/160 nM/125 nM and also inhibits PDGFRα/β with IC50 of 965 nM/9850 nM.

Catalog No.S1557

: Tel: +1-832-582-8158[email protected]

KRN 633 Chemical Structure
Molecular Weight: 416.86

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

KRN 633 is available in the following compound libraries:

Chemical Library (96-well) Inhibitor Library (96-well) Kinase Inhibitor Library (96-well) Tyrosine Kinase Inhibitor Library (96-Well)

Product Information

Compare VEGFR Inhibitors

Research Area
Research Area
Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

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S1042	Sunitinib Malate (Sutent)	<1 mg/mL	15 mg/mL	<1 mg/mL
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S1178	Regorafenib (BAY 73-4506)	<1 mg/mL	97 mg/mL	<1 mg/mL
S1119	XL-184 free base (Cabozantinib)	<1 mg/mL	100 mg/mL	<1 mg/mL
S1010	BIBF1120 (Vargatef)	<1 mg/mL	6 mg/mL	3 mg/mL
S1046	Vandetanib (Zactima)	<1 mg/mL	4 mg/mL	<1 mg/mL
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S1018	Dovitinib (TKI-258)	<1 mg/mL	30 mg/mL	<1 mg/mL
S1017	Cediranib (AZD2171)	<1 mg/mL	90 mg/mL	<1 mg/mL
S2161	RAF265 (CHIR-265)	<1 mg/mL	104 mg/mL	33 mg/mL
S1207	Tivozanib (AV-951)	<1 mg/mL	20 mg/mL	<1 mg/mL
S1470	TSU-68 (SU6668)	<1 mg/mL	62 mg/mL	<1 mg/mL
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S1361	MGCD-265	<1 mg/mL	104 mg/mL	<1 mg/mL
S2842	SAR131675	<1 mg/mL	30 mg/mL	<1 mg/mL
S1032	Motesanib Diphosphate (AMG-706)	114 mg/mL	114 mg/mL	<1 mg/mL
S2202	NVP-BHG712	<1 mg/mL	101 mg/mL	3 mg/mL
S2769	Dovitinib Dilactic acid (TKI258 Dilactic acid)	70 mg/mL	90 mg/mL	<1 mg/mL
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S1138	Brivanib alaninate (BMS-582664)	<1 mg/mL	88 mg/mL	88 mg/mL
S1486	AEE788 (NVP-AEE788)	<1 mg/mL	88 mg/mL	<1 mg/mL
S1557	KRN 633	<1 mg/mL	9 mg/mL	<1 mg/mL
S2221	Apatinib (YN968D1)	<1 mg/mL	22 mg/mL	<1 mg/mL
S2896	ZM 323881 HCl	<1 mg/mL	10 mg/mL	<1 mg/mL
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S2845	Semaxanib (SU5416)	<1 mg/mL	22 mg/mL	2 mg/mL
S2897	ZM 306416	<1 mg/mL	67 mg/mL	<1 mg/mL
S4001	Cabozantinib malate	<1 mg/mL	127 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Chemical Information Tech Support & FAQs

Biological Activity

Description	KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 170 nM/160 nM/125 nM and also inhibits PDGFRα/β with IC50 of 965 nM/9850 nM.
Targets	VEGFR1	VEGFR2	VEGFR3
IC50	170 nM	160 nM	125 nM ^[1]
In vitro	KRN 633, a novel quinazoline urea derivative, strongly inhibits VEGFR1, VEGFR2 and VEGFR3 receptors with IC50 values of 170 nM, 160 nM and 125 nM respectively. It shows lower inhibitory activity towards non-RTKs, such as PDGF receptor (PDGFRα and β, c-Kit, breast tumor kinase, and tunica interna endothelial cell kinase tyrosine kinases (IC50 = 965, 9850, 4330, 9200, and 9900 nM, respectively). KRN 633 potently inhibits ligand VEGF induced phosphorylation of VEGFR2 in HUVECs with an IC50 of 1.16 nM. KRN 633 also inhibits VEGF-dependent, but not bFGF-dependent, phosphorylation of the MAP kinases in endothelial cells, with IC50 values of 3.51 nM and 6.08 nM for ERK1 and ERK2, respectively. KRN633 has also been shown to inhibit the VEGF-driven proliferation of HUVECs with an IC50 of 14.9 nM, but it only suppresses FGF-driven proliferation at 3 μM weakly. ^[1] KRN 633 inhibits hypoxia-induced transcriptional activation of HIF-1α in a concentration-dependent manner with an IC50 of 3.79 μM, through the inhibition of both Akt and ERK phosphorylation signaling pathways. ^[2]
In vivo	Although not cytotoxic to various cancer cells in vitro, KRN633 exhibits excellent antitumor activity in vivo due to its inhibitory effect on tumor vessel formation and vascular permeability. Once-daily administration of KRN633 at 100 mg/kg/d produces significant tumor growth inhibition in A549, LC-6-LCK, HT29, Ls174T, LNCap and Du145 cells while twice-daily administration of KRN633 at 100 mg/kg induces ~90% growth inhibition of HT29 tumors. ^[1] Treatment of mid-pregnancy mice with KRN 633 (300 mg/kg, p.o.) reduces the blood supply to fetal tissues due to diminished vascularization in both placenta and fetal organs and consequently increases the risk of induction of intrauterine growth restriction (IUGR). ^[3]
Clinical Trials
Features

Protocol(Only for Reference)

Kinase Assay: ^[1]

Cell-Free Kinase Assays	Cell-free kinase assays are done to obtain IC50 values against a variety of recombinant VEGF receptors. KRN633 is tested at concentrations varying from 0.3 nM to 10 μM. All assays are done in quadruplicate with 1 μM ATP.

Cell Assay: ^[1]

Cell lines	A549, Ls174T, DU145, HT29, LNCap and PC-3 cell lines
Concentrations	Dissolved in DMSO, final concentrations 0.01 to 10 μM
Incubation Time	96 hours
Method	Cancer cells are plated in media containig 10% FBS and antibiotics, at densities known to permit exponential growth over the assay period. The cells are cultured for 24 hours before adding KRN633 (0.01 to 10 μM) or just the vehicle (0.1% DMSO in medium) and then grown for a further 96 hours. Cell viability is measured using WST-1 reagent.

Animal Study: ^[1]

Animal Models	A549, Ls174T, HT29, DU145, LNCap, PC-3 cells and LC-6-JCK are established in athymic mice (BALB/cA, Jcl-nu) and athymic rats (F344/N, Jcl-rnu), respectively.
Formulation	Suspended in vehicle (0.5% methylcellulose solution)
Dosages	20-100 mg/kg
Administration	Gavage once daily

References

Chemical Information

Download KRN 633 SDF

Molecular Weight (MW)	416.86
Formula	C₂₀H₂₁ClN₄O₄
CAS No.	286370-15-8
Synonyms	N/A

Solubility (25°C) DMSO 9 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name	1-(2-chloro-4-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-propylurea

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Research Area

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3Monday–Friday 9:00 AM–5:00 PM (Central Time)

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Related VEGFR Inhibitors

Linifanib (ABT-869)

Linifanib (ABT-869) is a novel, potent ATP-competitive RTK inhibitor for KDR, CSF-1R, Flt-1, Flt-3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM, 3 nM, and 66 nM respectively.
BIBF1120 (Vargatef)

BIBF1120 (Vargatef) is a potent inhibitor of VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Cediranib (AZD2171)

Cediranib (AZD2171) is a highly potent VEGFR2 inhibitor with IC50 of 0.5 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.
Dovitinib (TKI-258)

Dovitinib (TKI258, CHIR258) is a novel multi-target inhibitor for Flt3, c-Kit, FGFR1/3, VEGFR1/2/3, PDGFRα/β with IC50 of 1 nM, 2 nM, 8 nM/9 nM and 10 nM/13 nM/8 nM, 210 nM/27 nM respectively.
Motesanib Diphosphate (AMG-706)
Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3, PDGFR, c-Kit and Ret with IC50 of 2 nM/3 nM/6 nM, 84 nM, 8 nM and 59 nM, respectively.
Masitinib (AB1010)
Masitinib is a novel tyrosine kinases inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, resectively.
Brivanib (BMS-540215)

Brivanib is an ATP-competitive inhibitor against human VEGFR2 and FGFR with IC50 of 25 nM and 148 nM, respectively.
Vatalanib 2HCl (PTK787)

Vatalanib (PTK787) is an inhibitor of VEGFR2/KDR, Flt-1 and c-Kit with IC50 of 37 nM, 77 nM and 730 nM, respectively.
Foretinib (GSK1363089, XL880)

XL880 (GSK1363089, EXEL-2880) is an ATP-competitive inhibitor of MET and KDR with IC50 of 0.4 nM and 0.9 nM, respectively.
Brivanib alaninate (BMS-582664)

BMS-582664 is an oral VEGFR/FGFR inhibitor for VEGFR2, Flk1, VEGFR1 and FGFR1 with IC50 of 25 nM, 89 nM, 380 nM and 148 nM, respectively.

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KRN 633