SU6656

Catalog No.S7774

For research use only.

SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.

SU6656 Chemical Structure

CAS No. 330161-87-0

Selleck's SU6656 has been cited by 23 publications

Purity & Quality Control

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Biological Activity

Description SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.
Targets
YES [1] Lyn [1] Fyn [1] Src [1]
20 nM 130 nM 170 nM 280 nM
In vitro

In NIH 3T3 cells, SU 6656 inhibits the PDGF-stimulated S-phase induction with IC50 of 0.3-0.4 μM. SU 6656 also inhibits PDGF- and serum-mediated NIH 3T3 cell proliferation, as well as epidermal growth factor and colony-stimulating factor 1-stimulated DNA synthesis in normal and colony-stimulating factor 1 receptor transfected NIH 3T3 cells. SU6656 inhibits PDGF-stimulated c-Myc induction and ERK2 activation.[1] Pretreating Jurkat T-cells with SU 6656 leads to increased VSV-G luciferase activity.[2] SU 6656 impairs TGF-β-mediated upregulation of CTGF mRNA and protein in proximal epithelial HKC-8 cells, and also reduces CTGF expression in cells exposed to autocrine growth factors. SU 6656 interferes with Aurora kinase activity resulting in inhibition of cell division and formation multilobular nuclei.[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 insect cells M4GzemZ2dmO2aX;uJIF{e2G7 MUPJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KEircz30ZYdo\WRiUlXUJIV5eHKnc4Pl[EBqdiCVZkmgbY5{\WO2IHPlcIx{NCCLQ{WwQVAvPzdizszN Mm\kNlAyOTdyMES=
Assay
Methods Test Index PMID
Western blot phospho-c-Abl / c-Abl / phospho-c-Src / c-Src ; p-STAT3 / STAT3 ; p-p38 / p38 / p-CREB / CREB 23049975 19284568 30816523
Immunofluorescence p-p38 ; E-cadherin / Fibronectin 30816523 23246962
In vivo SU 6656 markedly and dose-dependently attenuates mecamylamine-induced experimental nicotine withdrawal syndrome in mice measured in terms of WSS and anxiety score.[4] Once-daily administration of SU 6656 (1.5, 3, and 6 mg/kg, i.p.) markedly and dose-dependently attenuates the naloxone-induced morphine withdrawal syndrome.[5]

Protocol (from reference)

Kinase Assay:[1]
  • Biochemical kinase assays for IC50 determination and kinetic studies:

    IC50 measurements are made using poly-Glu–Tyr (4:1), or, in the case of Lck, poly-Lys–Tyr (4:1) as a peptide substrate. The divalent cation is 20 mM MgCl2 (in the case of Src, Fyn, Yes, Lyn, Csk, Frk, or Abl) or 10 mM MnCl2 (in the case of FGFR1, IGF1R, Lck, or Met). The final ATP concentrations are as follows: Src, 10 μM; Fyn, 6 μM; Yes, 100 μM; Lyn, 2 μM; Csk, 10 μM; Frk, 10 μM; Abl, 4 μM; FGFR1, 10 μM; IGF1R, 2 μM; Lck, 2 μM; Met, 5 μM; PDGFR, 6 μM. IC50 measurements of PDGFRb autophosphorylation are determined on immunoprecipitated PDGFRb. Km values are calculated using the Eadie-Hofstee method.

Cell Research:[3]
  • Cell lines: HKC-8 cells
  • Concentrations: 5 μM
  • Incubation Time: 48 h
  • Method: HKC-8 cells are seeded at different cells densities (10,000 cells/cm2 and 50,000 cells/cm2) and cultured in the presence or absence of SU 6656 for 24 and 48 h. Bright field pictures of cells are recorded by Olympus CK40 microscope using Leica DC Viewer software.
  • (Only for Reference)
Animal Research:[4]
  • Animal Models: Inbred Swiss albino male mice
  • Dosages: 3 mg/kg
  • Administration: i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 74 mg/mL warmed
(199.21 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50%dd H2O
For best results, use promptly after mixing.

1.85mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 371.45
Formula

C19H21N3O3S

CAS No. 330161-87-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)S(=O)(=O)C1=CC2=C(C=C1)NC(=O)C2=CC3=CC4=C(N3)CCCC4

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

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

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