product name SU6656
Description: SU 6656 is a potent and 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 modulates CTGF (connective tissue growth factor) expression in an ERK-dependent manner. SU6656 induces caspase-independent cell death in FRO anaplastic thyroid carcinoma cells and therapeutic synergy in human synovial sarcoma growth, invasion and angiogenesis in vivo. In NIH 3T3 cell, SU6656 inhibits PDGF-/Src-driven mitogenesis and PDGF-stimulated c-Myc induction.
References: Mol Cell Biol. 2000 Dec;20(23):9018-27; Nicotine Tob Res. 2012 Apr;14(4):407-14.
371.45
Formula
C19H21N3O3S
CAS No.
330161-87-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 74 mg/mL (199.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
10% DMSO+dd H2O: 16 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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: 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 Assay: 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. |
|---|---|
| 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. 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. |
| Animal model | Inbred Swiss albino male mice |
| Formulation & Dosage | 10% DMSO in water; 1.5, 3, and 6 mg/kg; i.p. injection |
| References | Mol Cell Biol. 2000 Dec;20(23):9018-27; Nicotine Tob Res. 2012 Apr;14(4):407-14. |
