Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BX-912 是一种直接的,选择性的,ATP 竞争性的PDK1抑制剂,IC50值为 26 nM。它阻断肿瘤细胞 PDK1/Akt 信号转导,抑制多种肿瘤细胞株的锚定依赖性生长或诱导凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 419 | 现货 | ||
2 mg | ¥ 597 | 现货 | ||
5 mg | ¥ 788 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,660 | 现货 | ||
50 mg | ¥ 3,930 | 现货 | ||
100 mg | ¥ 5,730 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 818 | 现货 |
产品描述 | BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC etc. |
靶点活性 | PDK1:12 nM |
体外活性 | BX-912对ChcK1(IC50:0.83 μM),PKA(IC50:0.11 μM),c-kit(IC50:0.85 μM)和KDR(IC50:0.41 μM)有抑制作用。在肿瘤细胞中,BX-912可阻断PDK1/Akt信号,能抑制多种肿瘤细胞的贴壁依赖型生长(比如PC-3细胞)或者诱导凋亡。许多Akt活性升高的癌细胞株在软琼脂中对BX-912引起的生长抑制的敏感性比在组织培养塑料中高30倍,与PDK1/Akt信号通路的细胞生存功能一致,这对未贴壁细胞尤为重要。BX-912对PDK1酶活有显著的抑制效果, 但不影响AKT2活性(IC50>10 μM),故BX-912是PDK1的直接抑制剂。BX-912使含4 NDNA的MDA-468细胞数显著增多,并使细胞停在G2/M期。BX-912有效抑制细胞生长(IC50:0.32 μM)。BX-912(1 μM)对HCT-116细胞生长的抑制也十分有效(抑制率达96%)。 |
激酶实验 | Kinase assays: PDK1 is assayed in a direct kinase assay and a coupled assay format measuring PDK1- and PtdIns-3,4-P2-mediated activation of AKT2. For the coupled assay, the final assay mixture (60 μL) contained: 15 mM MOPS, pH 7.2, 1 mg/mL bovine serum albumin, 18 mM β-glycerol phosphate, 0.7 mM dithiothreitol, 3 mM EGTA, 10 mM MgOAc, 7.5 μM ATP, 0.2 μCi of [γ- 33P]ATP, 7.5 μM biotinylated peptide substrate (biotin-ARRRDGGGAQPFRPRAATF), 0.5 μL of PtdIns-3,4-P2-containing phospholipid vesicles, 60 pg of purified recombinant human PDK1, and 172 ng of purified recombinant human AKT2. After incubation for 2 hours at room temperature, the biotin-labeled peptide is captured from 10 μL of the assay mixture on streptavidin-coated SPA beads, and product formation is measured by scintillation proximity in a Wallac MicroBeta counter. The product formed is proportional to the time of incubation and to the amount of PDK1 and inactive AKT2 added. PDK1 is added at suboptimal levels so that the assay could sensitively detect inhibitors of AKT2 activation as well as direct inhibitor BX912 of PDK1 or AKT2. To measure PDK1 activity directly, the final assay mixture (60 μL) contained 50 mM Tris-HCl, pH 7.5, 0.1 mM EGTA, 0.1 mM EDTA, 0.1% β-mercaptoethanol, 1 mg/mL bovine serum albumin, 10 mM MgOAc, 10 μM ATP, 0.2 μCi of [γ-33P]ATP, 7.5 μM substrate peptide (H2N-ARRRGVTTKTFCGT), and 60 ng of purified recombinant human PDK1. After 4 hours at room temperature, 25 mM EDTA is added and a portion of the reaction mixture on P81 phosphocellulose paper is spotted. The filter paper is washed three times with 0.75% phosphoric acid and once with acetone. After drying, the filter-bound labeled peptide is quantified using a phosphorimager. |
细胞实验 | Cells such as MDA-468, MDA-453 are seeded at a low density (1.5-3 × 103 cells/well, 0.1 mL/well, 96-well plates) and are incubated overnight. BX912 treatments are made by adding 10 μL/well of the compound in 1% dimethyl sulfoxide and growth medium (final concentration of dimethyl sulfoxide, 0.1%), followed by brief shaking. Treated cells are incubated for 72 hours, and viability is measured by the addition of 10 μL of the metabolic dye WST-1. The WST-1 signal is read in a plate reader at 450 nm, and a no cell, or zero time cell, background is subtracted to calculate the net signal. (Only for Reference) |
分子量 | 471.35 |
分子式 | C20H23BrN8O |
CAS No. | 702674-56-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 87 mg/mL (184.6 mM)
Ethanol: 87 mg/mL (184.6 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.1216 mL | 10.6078 mL | 21.2157 mL | 53.0391 mL |
5 mM | 0.4243 mL | 2.1216 mL | 4.2431 mL | 10.6078 mL | |
10 mM | 0.2122 mL | 1.0608 mL | 2.1216 mL | 5.3039 mL | |
20 mM | 0.1061 mL | 0.5304 mL | 1.0608 mL | 2.652 mL | |
50 mM | 0.0424 mL | 0.2122 mL | 0.4243 mL | 1.0608 mL | |
100 mM | 0.0212 mL | 0.1061 mL | 0.2122 mL | 0.5304 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
BX-912 702674-56-4 Angiogenesis Apoptosis Cell Cycle/Checkpoint PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors PDK PKA CDK Chk VEGFR PDK-1 BX 912 inhibit BX912 Inhibitor inhibitor