KRN633 - CAS 286370-15-8
Catalog number: 286370-15-8
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
Inquire
Targets:
VEGFR
Description:
KRN633 is a potent and selective VEGFR inhibitor. which inhibits tyrosine phosphorylation of VEGFR-2 (IC50 = 1.16 nmol/L) in human umbilical vein endothelial cells. Selectivity profiling with recombinant tyrosine kinases showed that KRN633 is highly selective for VEGFR-1, -2, and -3. KRN633 inhibits tumor growth in several in vivo tumor xenograft models with diverse tissue origins, including lung, colon, and prostate, in athymic mice and rats. KRN633 also causes the regression of some well-established tumors and those that had regrown after the cessation of treatment. KRN633 was well tolerated and had no significant effects on body weight or the general health of the animals. KRN633 might be useful in the treatment of solid tumors and other diseases that depend on pathologic angiogenesis.
Publictions citing BOC Sciences Products
  • >> More
Purity:
0.98
Appearance:
Solid powder
Synonyms:
KRN633; KRN-633; KRN 633.
MSDS:
Inquire
1.KRN633, an inhibitor of vascular endothelial growth factor receptor tyrosine kinase, induces intrauterine growth restriction in mice.
Abe N1, Nakahara T, Morita A, Wada Y, Mori A, Sakamoto K, Nagamitsu T, Ishii K. Birth Defects Res B Dev Reprod Toxicol. 2013 Aug;98(4):297-303. doi: 10.1002/bdrb.21064. Epub 2013 Jun 18.
We previously reported that treatment with KRN633, a vascular endothelial growth factor receptor tyrosine kinase inhibitor, during mid-pregnancy caused intrauterine growth restriction resulting from impairment of blood vessel growth in the labyrinthine zone of the placenta and fetal organs. However, the relative sensitivities of blood vessels in the placenta and fetal organs to vascular endothelial growth factor (VEGF) inhibitors have not been determined. In this study, we aimed to examine the effects of KRN633 on the vasculatures of organs in mother mice and their newborn pups by immunohistochemical analysis. Pregnant mice were treated daily with KRN633 (5 mg/kg) either from embryonic day 13.5 (E13.5) to E17.5 or from E13.5 to the day of delivery. The weights of the pups of KRN633-treated mice were lower than those of the pups of vehicle-treated mothers. However, no significant difference in body weight was observed between the vehicle- and KRN633-treated mice.
2.Effects of pre- and post-natal treatment with KRN633, an inhibitor of vascular endothelial growth factor receptor tyrosine kinase, on retinal vascular development and patterning in mice.
Morita A1, Nakahara T2, Abe N1, Kurauchi Y1, Mori A1, Sakamoto K1, Nagamitsu T3, Ishii K1. Exp Eye Res. 2014 Mar;120:127-37. doi: 10.1016/j.exer.2014.01.009. Epub 2014 Jan 23.
The impaired function of angiogenic factors, including vascular endothelial growth factor (VEGF), during pregnancy is associated with preeclampsia and intrauterine growth restriction. To determine how the attenuation of VEGF signals during retinal vascular development affects retinal vascular growth and patterns, we examined the effects of pre- and post-natal treatment of mice with KRN633, a VEGF receptor tyrosine kinase inhibitor, on retinal vascular development and structure. Delays in retinal vascular development were observed in the pups of mother mice that were treated daily with KRN633 (5 mg/kg/day) from embryonic day 13.5 until the day of delivery. A more marked delay was seen in pups treated with the inhibitor (5 mg/kg/day) on the day of birth and on the following day. Pups treated postnatally with KRN633 showed abnormal retinal vascular patterns, such as highly dense capillary networks and decreased numbers of central arteries and veins.
3.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.
Morita A1, Nakahara T, Abe N, Kurauchi Y, Mori A, Sakamoto K, Nagamitsu T, Ishii K. Birth Defects Res B Dev Reprod Toxicol. 2014 Aug;101(4):293-9. doi: 10.1002/bdrb.21112. Epub 2014 May 15.
We previously reported that treatment of mid-pregnant mice with KRN633, a vascular endothelial growth factor receptor tyrosine kinase inhibitor, caused fetal growth restriction resulting from diminished vascularization in the placenta and fetal organs. In this study, we examined how the treatment of mid-pregnant mice with KRN633 affects the development and morphology of vascular components (endothelial cells, pericytes, and basement membrane) in the retinas of their newborn pups. Pregnant mice were treated with KRN633 (5 mg/kg) once daily from embryonic day 13.5 until the day of delivery. Vascular components were examined using immunohistochemistry with specific markers for each component. Radial vascular growth in the retina was slightly delayed until postnatal day 4 (P4) in the newborn pups of KRN633-treated mothers. On P8, compared with the pups of control mothers, the pups of KRN633-treated mothers exhibited decreased numbers of central arteries and veins and abnormal branching of the central arteries.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related VEGFR Products


CAS 219580-11-7 PD173074

PD173074
(CAS: 219580-11-7)

PD173074 is a small-molecule FGFR3-selective tyrosine kinase inhibitor (TKI), as a therapeutic modality using eight UC cell lines. PD173074 suppressed cell prol...

CAS 408502-06-7 KDR-in-4

KDR-in-4
(CAS: 408502-06-7)

A potent kinase insert domain-containing receptor (KDR/VEGFR2) inhibitor (IC50= 7 nM)

Anlotinib Dihydrochloride
(CAS: 1360460-82-7)

Anlotinib Dihydrochloride is a novel multi-target tyrosine kinase inhibitor with potential antineoplastic and anti-angiogenic activities, which was designed to ...

CAS 639858-32-5 BMS 605541

BMS 605541
(CAS: 639858-32-5)

BMS 605541 is a potent and ATP-competitive VEGFR-2 inhibitor (IC50 = 23 nM) displaying >10-fold selectivity for VEGFR-2 over VEGFR-1. It exhibits antitumor acti...

CAS 886563-25-3 ZK-261991

ZK-261991
(CAS: 886563-25-3)

ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC50 of 5 nM for VEGFR2. The high efficacy, including tumour regression in established tum...

CAS 656247-18-6 BIBF 1120 esylate

BIBF 1120 esylate
(CAS: 656247-18-6)

Nintedanib esylate is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β.

CAS 1140909-48-3 Cabozantinib malate (XL184)

Cabozantinib malate (XL184)
(CAS: 1140909-48-3)

Cabozantinib malate is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL w...

CAS 212141-54-3 Vatalanib

Vatalanib
(CAS: 212141-54-3)

Vatalanib, also called as PTK 787 or CGP 797870, is a small molecule that interacts reversibly and competitively at the ATP-binding site of the receptor tyrosin...

CAS 857876-30-3 Motesanib Diphosphate

Motesanib Diphosphate
(CAS: 857876-30-3)

Motesanib Diphosphate is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more...

CAS 849217-68-1 Cabozantinib

Cabozantinib
(CAS: 849217-68-1)

Cabozantinib is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 1...

CAS 900573-88-8 JI-101

JI-101
(CAS: 900573-88-8)

JI-101 is an orally active inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFRb), and the e...

CAS 557795-19-4 Sunitinib

Sunitinib
(CAS: 557795-19-4)

Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.

CAS 164658-13-3 CGP60474

CGP60474
(CAS: 164658-13-3)

CGP60474 is a promising inhibitor of PKC with a high degree of selectivity versus other serine/threonine and tyrosine kinases and show competitive kinetics rela...

Ramucirumab
(CAS: 947687-13-0)

Ramucirumab is a human IgG1 monoclonal antibody developed by ImClone Systems Inc to treat solid tumors. It has been approved by FDA for the treatment of advance...

CAS 882531-87-5 R1530

R1530
(CAS: 882531-87-5)

R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (...

CAS 867331-82-6 TG 100801

TG 100801
(CAS: 867331-82-6)

TG 100801 is the prodrug of TG 100572, which is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kin...

CAS 338992-53-3 Vandetanib trifluoroacetate

Vandetanib trifluoroacetate
(CAS: 338992-53-3)

Vandetanib is an anti-cancer drug that is used for the treatment of certain tumours of thethyroid gland. It acts as a kinase inhibitor of a number of cell recep...

CAS 252916-29-3 Orantinib

Orantinib
(CAS: 252916-29-3)

TSU-68 (SU6668; Orantinib) is a novel multiple receptor tyrosine kinase inhibitor with IC50 of 2.1 μM, 8 nM and 1.2 μM for VEGF-R1, PDGF-Rβ and FGF-R1, respecti...

CAS 38101-59-6 H-Glu-Trp-OH

H-Glu-Trp-OH
(CAS: 38101-59-6)

H-Glu-Trp-OH inhibits VEGF, which may inhibit angiogenesis.

CAS 1174046-72-0 BMS-794833

BMS-794833
(CAS: 1174046-72-0)

BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7 nM/15 nM.

Chemical Structure

CAS 286370-15-8 KRN633

Quick Inquiry

Verification code

Featured Items