Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Taselisib (GDC-0032) 是 PI3K 抑制剂,靶向作用于突变 PI3KCA。它能够抑制 PI3Kα (IC50:0.29 nM),PI3Kβ (IC50:0.91 nM) 和 PI3Kγ (IC50:0.97 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 247 | 现货 | ||
2 mg | ¥ 346 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 913 | 现货 | ||
25 mg | ¥ 1,460 | 现货 | ||
50 mg | ¥ 1,980 | 现货 | ||
100 mg | ¥ 3,730 | 现货 | ||
200 mg | ¥ 5,360 | 现货 | ||
500 mg | ¥ 8,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 588 | 现货 |
产品描述 | Taselisib (GDC-0032) is an orally bioavailable inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) alpha isoform (PIK3CA), with potential antineoplastic activity. |
靶点活性 | PI3Kγ:0.97 nM(Ki), PI3Kα:0.29 nM(Ki), PI3Kβ:9.1 nM(Ki), PI3Kδ:0.12 nM(Ki), C2β:292 nM |
体外活性 | GDC-0032与氟维司群联用,增强氟维司群活性,导致肿瘤消退和肿瘤生长延迟(91%肿瘤生长抑制(TGI)).此外,GDC-0032与他莫昔芬联用,增强他莫昔芬在体内的效力,GDC-0032的肿瘤生长抑制率为102%.GDC-0032药代动力学大约与剂量成比例并且与时间无关,平均t1/2为40小时. |
体内活性 | 临床前期数据表明,GDC-0032具有增加PI3Kα同种型(PIK3CA)突变体和HER2扩增的癌细胞系的活性。GDC-0032抑制MCF7-neo/HER2 细胞增殖,IC50为2.5 nM。GDC-0032是I类PI3Kα,δ和γ同种型的口服生物可利用的,有效的和选择性的抑制剂,相对于PI3Kα同种型,其对PI3Kβ同种型抑制率低30倍。 |
激酶实验 | Characterization of Biochemical and Cellular Activity in Vitro: Enzymatic activity of the class I PI3K isoforms is measured using a fluorescence polarization assay that monitors formation of the product 3,4,5-inositoltriphosphate molecule as it competes with fluorescently labeled PIP3 for binding to the GRP-1 pleckstrin homology domain protein. An increase in phosphatidyl inositide-3-phosphate product results in a decrease in fluorescence polarization signal as the labeled fluorophore is displaced from the GRP-1 protein binding site. Class I PI3K isoforms are expressed and purified as heterodimeric recombinant proteins. Tetramethylrhodamine-labeled PIP3 (TAMRA-PIP3), di-C8-PIP2, and PIP3 detection reagents are purchased from Echelon Biosciences. PI3Kα is assayed under initial rate conditions in the presence of 10 mM Tris (pH 7.5), 25 μM ATP, 9.75 μM PIP2, 5% glycerol, 4 mM MgCl2, 50 mM NaCl, 0.05% (v/v) Chaps, 1 mM dithiothreitol, and 2% (v/v) DMSO at 60 ng/mL. After assay for 30 min at 25 °C, reactions are terminated with a final concentration of 9 mM EDTA, 4.5 nM TAMRA-PIP3, and 4.2 μg/mL GRP-1 detector protein before reading fluorescence polarization on an Envision plate reader. IC50 values are calculated from the fit of the dose-response curves to a 4-parameter equation. Each reported value is an average of three experiments, and all have a standard deviation less than one geometric mean. |
细胞实验 | GDC-0032 is dissolved in DMSO. Cells are seeded in replicates of 6 in 96-well plates with 500 to 5,000 cells/well overnight and then treated with GDC-0032. After 4 days, the media are removed and the cells are fixed with 4% glutaraldehyde for 30 minutes. Fixed cells are stained with 0.1% crystal violet for 2 minutes, then washed, and dissolved in 10% acetic acid. |
别名 | RG-7604, GDC-0032 |
分子量 | 460.53 |
分子式 | C24H28N8O2 |
CAS No. | 1282512-48-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 70 mg/mL (151.99 mM), Heating is recommended.
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1714 mL | 10.8571 mL | 21.7141 mL | 54.2853 mL |
5 mM | 0.4343 mL | 2.1714 mL | 4.3428 mL | 10.8571 mL | |
10 mM | 0.2171 mL | 1.0857 mL | 2.1714 mL | 5.4285 mL | |
20 mM | 0.1086 mL | 0.5429 mL | 1.0857 mL | 2.7143 mL | |
50 mM | 0.0434 mL | 0.2171 mL | 0.4343 mL | 1.0857 mL | |
100 mM | 0.0217 mL | 0.1086 mL | 0.2171 mL | 0.5429 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。
Taselisib 1282512-48-4 Metabolism PI3K/Akt/mTOR signaling PI3K Carbonic Anhydrase RG7604 inhibit RG-7604 Inhibitor GDC0032 Phosphoinositide 3-kinase GDC 0032 RG 7604 GDC-0032 inhibitor