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SU6656

SU6656

产品编号 T6997   CAS 330161-87-0

SU6656 是Src 家族激酶抑制剂,抑制 Src,Yes,Lyn,Fyn 的IC50分别为 280,20,130,170 nM。它还能抑制p-AKT。它可抑制FAK Y576/577、 Y925、Y861位点的磷酸化。

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SU6656 Chemical Structure
SU6656, CAS 330161-87-0
规格 价格/CNY 货期 数量
1 mg ¥ 279 现货
2 mg ¥ 397 现货
5 mg ¥ 655 现货
10 mg ¥ 987 现货
25 mg ¥ 1,980 现货
50 mg ¥ 3,250 现货
100 mg ¥ 4,750 现货
1 mL * 10 mM (in DMSO) ¥ 719 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: SU6656 (T6997)
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纯度: 98.21%
纯度: 97%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 SU 6656 is a selective inhibitor of Src family kinases, with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.
靶点活性 YES:20 nM, Fyn:170 nM, Lyn:130 nM, Src:280 nM
体外活性 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]
体内活性 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]
激酶实验 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 ?nal 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.
细胞实验 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 ?eld pictures of cells are recorded by Olympus CK40 microscope using Leica DC Viewer software.(Only for Reference)
分子量 371.45
分子式 C19H21N3O3S
CAS No. 330161-87-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 69 mg/mL (185.8 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6922 mL 13.4608 mL 26.9215 mL 67.3038 mL
5 mM 0.5384 mL 2.6922 mL 5.3843 mL 13.4608 mL
10 mM 0.2692 mL 1.3461 mL 2.6922 mL 6.7304 mL
20 mM 0.1346 mL 0.673 mL 1.3461 mL 3.3652 mL
50 mM 0.0538 mL 0.2692 mL 0.5384 mL 1.3461 mL
100 mM 0.0269 mL 0.1346 mL 0.2692 mL 0.673 mL

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TargetMol Library Books参考文献

1. Blake RA, et al. Mol Cell Biol. 2000, 20(23), 9018-9027. 2. McCarthy SD, et al. J Acquir Immune Defic Syndr.2014, 66(2), 118-126. 3. Cicha I, et al. Int J Biochem Cell Biol. 2014 Jan;46:39-48. 4. Rehni AK, et al. Nicotine Tob Res. 2012, 14(4), 407-414. 5. Rehni AK, et al. Behav Pharmacol. 2011, 22(2), doi: 10.1097/FBP.
PF-562271 hydrochloride YH-306 FAK-IN-10 5α-Hydroxycostic acid Chloropyramine hydrochloride (R)-Fangchinoline GSK2256098 Y15

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 激酶抑制剂库 酪氨酸激酶分子库 抗胰腺癌化合物库 活性脂质化合物库 NO PAINS 化合物库 抗乳腺癌化合物库 抗肝癌化合物库 抗前列腺癌化合物库 神经再生化合物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

SU6656 330161-87-0 Angiogenesis Cytoskeletal Signaling PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors FAK Akt Src PTK2 protein tyrosine kinase 2 SU-6656 Focal adhesion kinase PTK2 SU 6656 Inhibitor Protein kinase B PKB inhibit inhibitor

 

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