SU14813 maleate

VEGFR/PDGFR/Kit/FLT-3 inhibitor CAS# 849643-15-8

SU14813 maleate

Catalog No. BCC1973----Order now to get a substantial discount!

Product Name & Size Price Stock
SU14813 maleate: 5mg $127 In Stock
SU14813 maleate: 10mg Please Inquire In Stock
SU14813 maleate: 20mg Please Inquire Please Inquire
SU14813 maleate: 50mg Please Inquire Please Inquire
SU14813 maleate: 100mg Please Inquire Please Inquire
SU14813 maleate: 200mg Please Inquire Please Inquire
SU14813 maleate: 500mg Please Inquire Please Inquire
SU14813 maleate: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of SU14813 maleate

Number of papers citing our products

Chemical structure

SU14813 maleate

3D structure

Chemical Properties of SU14813 maleate

Cas No. 849643-15-8 SDF Download SDF
PubChem ID 11353475 Appearance Powder
Formula C27H31FN4O8 M.Wt 558.56
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (179.03 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (Z)-but-2-enedioic acid;5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
SMILES CC1=C(NC(=C1C(=O)NCC(CN2CCOCC2)O)C)C=C3C4=C(C=CC(=C4)F)NC3=O.C(=CC(=O)O)C(=O)O
Standard InChIKey PQPBIMIFGPFTNF-FYOMJGPWSA-N
Standard InChI InChI=1S/C23H27FN4O4.C4H4O4/c1-13-20(10-18-17-9-15(24)3-4-19(17)27-22(18)30)26-14(2)21(13)23(31)25-11-16(29)12-28-5-7-32-8-6-28;5-3(6)1-2-4(7)8/h3-4,9-10,16,26,29H,5-8,11-12H2,1-2H3,(H,25,31)(H,27,30);1-2H,(H,5,6)(H,7,8)/b18-10-;2-1-/t16-;/m0./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of SU14813 maleate

DescriptionSU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.In Vitro:SU14813 inhibits ligand-dependent and ligand-independent proliferation, migration, and survival of endothelial cells and/or tumor cells expressing these targets. SU14813 inhibits cellular ligand-dependent phosphorylation of VEGFR-2 (transfected NIH 3T3 cells), PDGFR-β (transfected NIH 3T3 cells), KIT (Mo7e cells), and FLT3-internal tandem duplication (FLT3-ITD; MV4;11 cells) as well as FMS/CSF1R (transfected NIH 3T3 cells). SU14813 inhibits VEGFR-2, PDGFR-β, and KIT phosphorylation in porcine aorta endothelial cells overexpressing these targets, with cellular IC50 values of 5.2, 9.9, and 11.2 nM, respectively. SU14813 inhibits the growth of U-118MG with an IC50 of 50 to 100 nM[1].In Vivo:SU14813 inhibits VEGFR-2, PDGFR-β, and FLT3 phosphorylation in xenograft tumors in a dose- and time-dependent fashion. The plasma concentration required for in vivo target inhibition is estimated to be 100 to 200 ng/mL. Used as monotherapy, SU14813 exhibits broad and potent antitumor activity resulting in regression, growth arrest, or substantially reduced growth of various established xenografts derived from human or rat tumor cell lines. Treatment in combination with docetaxel significantly enhances both the inhibition of primary tumor growth and the survival of the tumor-bearing mice compared with administration of either agent alone[1].

References:
[1]. Patyna S, et al. SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol Cancer Ther. 2006 Jul;5(7):1774-82.

Protocol

Cell Assay [1]
The effect of SU14813 on endothelial cell survival is evaluated. Passages 4 to 5 human umbilical vein endothelial cells are grown to subconfluency in EGM2 medium containing 10% FBS, endothelial cell growth supplement, and 10 μg/mL sodium heparin. The cells are seeded in 96-well plates at 10,000 per well in F12K medium and 10% FBS. The next day, cells are starved for 18 hours in F12K+1% FBS and then incubated with SU14813 in various concentrations. 45 minutes later, 20 ng/mL growth factor [VEGF or basic fibroblast growth factor (bFGF)] is introduced into the assay. Three days later, cell numbers are determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay[1].

Animal Administration [1]
Mouse: SU14813 is evaluated for its efficacy and synergism in combination with the microtubule inhibitor docetaxel in docetaxel-resistant murine LLC model. SU14813 is administered p.o. twice daily (BID) at doses of 10, 40, 80, or 120 mg/kg beginning on day 5 after tumor implantation. Docetaxel 40 mg/kg (mouse maximum tolerated dose) is administered i.v. thrice weekly also beginning on day 5 after tumor implantation[1].

References:
[1]. Patyna S, et al. SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol Cancer Ther. 2006 Jul;5(7):1774-82.

SU14813 maleate Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

SU14813 maleate Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of SU14813 maleate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.7903 mL 8.9516 mL 17.9032 mL 35.8064 mL 44.7579 mL
5 mM 0.3581 mL 1.7903 mL 3.5806 mL 7.1613 mL 8.9516 mL
10 mM 0.179 mL 0.8952 mL 1.7903 mL 3.5806 mL 4.4758 mL
50 mM 0.0358 mL 0.179 mL 0.3581 mL 0.7161 mL 0.8952 mL
100 mM 0.0179 mL 0.0895 mL 0.179 mL 0.3581 mL 0.4476 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on SU14813 maleate

SU14813 maleate is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), Kit, and fms-like tyrosine kinase 3 (FLT-3).

Featured Products
New Products
 

Description

SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.

Keywords:

SU14813 maleate,849643-15-8,Natural Products,VEGFR, buy SU14813 maleate , SU14813 maleate supplier , purchase SU14813 maleate , SU14813 maleate cost , SU14813 maleate manufacturer , order SU14813 maleate , high purity SU14813 maleate

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: