SU5402 is a potent and selective small molecular vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor. SU5402 inhibits embryonic left-right determination and exhibits potent anticancer activity in vitro and in vivo.
|Cell lines||KMS11, UTMC-2, LP1, OPM1, OPM2, KHM11, JJN3, RPMI8226, EJM, K620, H929, U266 and OCI-My5 cell lines|
|Preparation method||KMS11 (provided by MasayoshiNamba), UTMC-2, LP1, OPM1, OPM2, KHM11, JJN3, RPMI8226, EJM, K620, H929 (provided by Leif Bergsagel), U266 and OCI-My5 (provided by Robert Hawley) were grown in Iscove’s modified Dulbecco’s medium (IMDM) supplemented with 10% fetal calf serum (FCS) and 1% Gibco antimycotic/antibiotic (Invitrogen Canada, Ontario, Canada). For proliferation assays, cells were washed and plated in triplicate in IMDM plus 5% FCS and incubated with various concentrations of SU5402. Cells were then analysed by MTT [3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide] assay (Boehringer Mannheim, Mannheim, Germany) according to the manufacturer’s protocol.|
|Incubation time||48 h|
|Animal models||Spinal cords lesions of zebrafish|
|Dosages||1 μl of 5 μg/μl|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Source||Stem Cell Reports (2017). SU5402, Figure1 . (AbMole Bioscience)|
|Cell Lines||The mouse ESC lines J1 (ATCC SCRC-1010), CCE, and Jmjd2c KO|
|Results||FGFR inhibition (FGFRi) by SU5402 had little effect compared with LIF (Figure 1A). A two-inhibitor combination (PD0325901 and CHIR99021) and a threeinhibitor combination (PD0325901, CHIR99021, and SU5402) produced robust AP staining of ESCs with a compact colony morphology.|
Stem Cell Reports. 2017 May 9;8(5): 1312–1328.
2i Maintains a Naive Ground State in ESCs through Two Distinct Epigenetic Mechanisms
SU5402 purchased from AbMole
Nectin-1 binds and signals through the fibroblast growth factor receptor.
Bojesen KB, et al. J Biol Chem. 2012 Oct 26;287(44):37420-33. PMID: 22955284.
Characterization and expressional analysis of Dleu7 during Xenopus tropicalis embryogenesis.
Zhu X, et al. Gene. 2012 Nov 1;509(1):77-84. PMID: 22939871.
A retrospective analysis of germline competence in rat embryonic stem cell lines.
Hirabayashi M, et al. Transgenic Res. 2013 Apr;22(2):411-6. PMID: 22875289.
FGF-induced vesicular release of Sonic hedgehog and retinoic acid in leftward nodal flow is critical for left-right determination.
Tanaka Y, et al. Nature. 2005 May 12;435(7039):172-7. PMID: 15889083.
|Related VEGFR/PDGFR Products|
Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous KIT mutation, D816V in KIT Exon 17 (IC50 = 0.5 nM).
|Nintedanib Ethanesulfonate Salt
BIBF 1120 esylate is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
|Pazopanib HCl (GW786034 )
Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.
|Dovitinib (TKI-258) Dilactic Acid
Dovitinib Dilactic acid (TKI258 Dilactic acid) is the Dilactic acid of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM.
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