SU6656 | Src inhibitor | CAS 330161-87-0

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Quality Control

Batch: Purity: 99.84%

99.84

Related Targets	EGFR VEGFR JAK PDGFR FGFR HIF FLT FLT3 HER2 Bcr-Abl
Other Src Products	WH-4-023 Saracatinib (AZD0530) PP2 (AGL 1879) PP1 Src Inhibitor 1 RK 24466 Myristic Acid eCF506 Tolimidone (MLR-1023) UM-164

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
Sf9 insect cells	Function assay				Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells, IC50=0.77 μM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 74 mg/mL (199.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.850mg/ml (4.98mM)	Taking the 1 mL working solution as an example, add 50 μL of 37 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	371.45	Formula	C₁₉H₂₁N₃O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	330161-87-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CN(C)S(=O)(=O)C1=CC2=C(C=C1)NC(=O)C2=CC3=CC4=C(N3)CCCC4

Mechanism of Action

Targets/IC₅₀/Ki	YES 20 nM Lyn 130 nM Fyn 170 nM Src 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. Pretreating Jurkat T-cells with SU 6656 leads to increased VSV-G luciferase activity. 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.
Kinase Assay	Biochemical kinase assays for IC50 determination and kinetic studies
Kinase Assay	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.
In vivo	SU 6656 markedly and dose-dependently attenuates -induced experimental nicotine withdrawal syndrome in mice measured in terms of WSS and anxiety score.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11074000/ [2] https://pubmed.ncbi.nlm.nih.gov/24413044/ [3] https://pubmed.ncbi.nlm.nih.gov/24275091/ [4] https://pubmed.ncbi.nlm.nih.gov/22102627/ [5] https://pubmed.ncbi.nlm.nih.gov/21285874/

Applications

Methods	Biomarkers	Images	PMID
Western blot	phospho-c-Abl / c-Abl / phospho-c-Src / c-Src p-p38 / p38 / p-CREB / CREB p-STAT3 / STAT3		23049975
Immunofluorescence	E-cadherin / Fibronectin p-p38		23246962