NVP-BAG956
(Synonyms: 2-甲基-2-[4-[2-甲基-8-[(吡啶-3-基)乙炔基]咪唑并[4,5-C]喹啉-1-基]苯基]丙腈,BAG 956) 目录号 : GC13725
A dual PDK1 and class I PI3K inhibitor
Cas No.:853910-02-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | One day after plating (7×103 cells/cm2), melanoma cells (A2058, B16F1, B16F10, C32, HBL, Malme, Malme3M, NA8, SKMel2, SKMel23, A375, Hs294T, WM35, and 1205lu cells) are exposed to LY294002 (25 μM), Wortmannin (500 nM), NVP-BAG956 (1 μM), NVP-BBD130 (1 μM), NVP-BEZ235 (1 μM), and ZSTK474 (1 μM), and Rapamycin (100 nM). Compound concentrations are set 2 log units above the IC50 in vitro to ensure full PI3K inhibition, except for the μM inhibitor LY294002. Cells are trypsinized and counted, and the volume is quantified using a Casy Counter and Analyser. To determine the nuclear volume, cells are resuspended in CASYton containing 0.5% Triton X-100, followed by repetitive pipetting (8×), before volume measurements[1]. |
References: [1]. Marone R, et al. Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors. Mol Cancer Res. 2009 Apr;7(4):601-13. | |
NVP-BAG956 is an ATP-competitive PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
NVP-BAG956 also inhibits PDK1 with an IC50 of 240/260 nM. NVP-BAG956 also inhibits VEGFR1 with an IC50 of 2.56±0.56 μM. NVP-BAG956 blocks phosphorylation of PKB/Akt in A2058 cells with an IC50 value of 67±25 nM. Inhibition of PKB/Akt phosphorylation correlated with loss of A2058 cell proliferation for NVP-BAG956 (IC50=290±20 nM). In the presence of NVP-BAG956, A2058 cells are only able to exit G2-M and then remain in G1. The p27 Kip1 expression is clearly induced by NVP-BAG956 in A2058 cells but not in C32 cells[1].
References:
[1]. Marone R, et al. Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors. Mol Cancer Res. 2009 Apr;7(4):601-13.
| Cas No. | 853910-02-8 | SDF | |
| 别名 | 2-甲基-2-[4-[2-甲基-8-[(吡啶-3-基)乙炔基]咪唑并[4,5-C]喹啉-1-基]苯基]丙腈,BAG 956 | ||
| 化学名 | 2-methyl-2-(4-(2-methyl-8-(pyridin-3-ylethynyl)-1H-imidazo[4,5-c]quinolin-1-yl)phenyl)propanenitrile | ||
| Canonical SMILES | CC1=NC2=CN=C3C=CC(C#CC4=CN=CC=C4)=CC3=C2N1C5=CC=C(C(C)(C#N)C)C=C5 | ||
| 分子式 | C28H21N5 | 分子量 | 427.5 |
| 溶解度 | DMSO: 20 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3392 mL | 11.6959 mL | 23.3918 mL |
| 5 mM | 0.4678 mL | 2.3392 mL | 4.6784 mL |
| 10 mM | 0.2339 mL | 1.1696 mL | 2.3392 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。