受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C19H21N3O3S |
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分子量 | 371.45 | CAS No. | 330161-87-0 | ||||
Solubility (25°C)* | 体外 | DMSO (warmed with 50ºC water bath) | 74 mg/mL (199.21 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * 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. |
製品説明 | 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. |
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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] |
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] |
キナーゼアッセイ | Biochemical kinase assays for IC50 determination and kinetic studies | |
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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. | ||
細胞アッセイ | 細胞株 | HKC-8 cells |
濃度 | 5 μM | |
反応時間 | 48 h | |
実験の流れ | 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. |
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動物実験 | 動物モデル | Inbred Swiss albino male mice |
投薬量 | 3 mg/kg | |
投与方法 | i.p. |
, , Exp Cell Res, 2017, 358(2):360-368
Data from [Data independently produced by , , J Virol, 2015, 90(1):9-21]
Data from [Data independently produced by , , J Biol Chem, 2014, 289(18):12313-29.]
CD28-CAR-T cell activation through FYN kinase signaling rather than LCK enhances therapeutic performance [ Cell Rep Med, 2023, S2666-3791(23)00002-2] | PubMed: 36696897 |
Direct regulation of FNIP1 and FNIP2 by MEF2 sustains MTORC1 activation and tumor progression in pancreatic cancer [ Autophagy, 2023, 1-20.] | PubMed: 37772772 |
Drug-repurposing screen on patient-derived organoids identifies therapy-induced vulnerability in KRAS-mutant colon cancer [ Cell Rep, 2023, 42(4):112324] | PubMed: 37000626 |
Adjuvant activity of tubeimosides by mediating the local immune microenvironment [ Front Immunol, 2023, 14:1108244] | PubMed: 36845089 |
Inhibition of Oncogenic Src Ameliorates Silica-Induced Pulmonary Fibrosis via PI3K/AKT Pathway [ Int J Mol Sci, 2023, 24(1)774] | PubMed: 36614217 |
Dynamic changes in O-GlcNAcylation regulate osteoclast differentiation and bone loss via nucleoporin 153 [ Bone Res, 2022, 10(1):51] | PubMed: 35879285 |
The Lectin LecB Induces Patches with Basolateral Characteristics at the Apical Membrane to Promote Pseudomonas aeruginosa Host Cell Invasion [ mBio, 2022, 13(3):e0081922] | PubMed: 35491830 |
Disruption of FOXO3a-miRNA feedback inhibition of IGF2/IGF-1R/IRS1 signaling confers Herceptin resistance in HER2-positive breast cancer [ Nat Commun, 2021, 12(1):2699] | PubMed: 33976188 |
A novel patient stratification strategy to enhance the therapeutic efficacy of dasatinib in glioblastoma [ Neuro Oncol, 2021, noab158] | PubMed: 34232320 |
Siglec-8 Signals Through a Non-Canonical Pathway to Cause Human Eosinophil Death In Vitro [ Front Immunol, 2021, 12:737988] | PubMed: 34721399 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。