NVP-BAG956
Based on 1 Customer Validation
NVP-BAG956 is an ATP-competitive PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
For research use only. We do not sell to patients.
- Purity: 98.23%
- CAS No.: 853910-02-8
- Formula: C28H21N5
- Molecular Weight:427.50
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
-
Differentiation Inducing Compound Library
HY-L038
-
Oxygen Sensing Compound Library
HY-L045
-
Glycolysis Compound Library
HY-L058
-
Cytoskeleton Compound Library
HY-L060
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Lung Cancer Compound Library
HY-L075
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Anti-Blood Cancer Compound Library
HY-L079
-
Anti-Cancer Metabolism Compound Library
HY-L083
-
Anti-Obesity Compound Library
HY-L087
-
Angiogenesis-Related Compound Library
HY-L088
-
Glucose Metabolism Compound Library
HY-L092
-
Anti-Liver Cancer Compound Library
HY-L101
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Anti-Pulmonary Fibrosis Compound Library
HY-L125
-
Cancer Stem Cells Compound Library
HY-L135
-
Pain-Related Compound Library
HY-L139
-
Membrane Protein-targeted Compound Library
HY-L149
-
Anti-Hematopathy Compound Library
HY-L171
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Anti-Fibrosis Compound Library
HY-L185
-
Anti-Brain Cancer Compound Library
HY-L188
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Anti-Rheumatic Arthritis Compound Library
HY-L210
-
Posttranslational Modification Library
HY-L226
-
Lactylation Compound Library
HY-L249
-
Alkyne Compound Library
HY-L258
-
Kinase Inhibitor Library
HY-L009
-
PI3K/Akt/mTOR Compound Library
HY-L015
-
Stem Cell Signaling Compound Library
HY-L017
-
Anti-Cancer Compound Library
HY-L025
-
Autophagy Compound Library
HY-L029
-
Anti-Aging Compound Library
HY-L034
Biological Activity
|
PI3Kδ 35 nM (IC50) |
PI3Kα 56 nM (IC50) |
PI3Kγ 117 nM (IC50) |
PI3Kβ 446 nM (IC50) |
PDK1 240 nM (IC50) |
VEGFR1 2.56 μM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 853910-02-8
-
Appearance Solid
-
Molecular Weight 427.50
-
Formula C28H21N5
-
Color Off-white to light yellow
-
SMILES
CC1=NC2=C(C3=CC(C#CC4=CC=CN=C4)=CC=C3N=C2)N1C5=CC=C(C=C5)C(C#N)(C)C
-
Synonyms
BAG 956
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (116.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.85 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (281 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3392 mL | 11.6959 mL | 23.3918 mL | 58.4795 mL |
| 5 mM | 0.4678 mL | 2.3392 mL | 4.6784 mL | 11.6959 mL | |
| 10 mM | 0.2339 mL | 1.1696 mL | 2.3392 mL | 5.8480 mL | |
| 15 mM | 0.1559 mL | 0.7797 mL | 1.5595 mL | 3.8986 mL | |
| 20 mM | 0.1170 mL | 0.5848 mL | 1.1696 mL | 2.9240 mL | |
| 25 mM | 0.0936 mL | 0.4678 mL | 0.9357 mL | 2.3392 mL | |
| 30 mM | 0.0780 mL | 0.3899 mL | 0.7797 mL | 1.9493 mL | |
| 40 mM | 0.0585 mL | 0.2924 mL | 0.5848 mL | 1.4620 mL | |
| 50 mM | 0.0468 mL | 0.2339 mL | 0.4678 mL | 1.1696 mL | |
| 60 mM | 0.0390 mL | 0.1949 mL | 0.3899 mL | 0.9747 mL | |
| 80 mM | 0.0292 mL | 0.1462 mL | 0.2924 mL | 0.7310 mL | |
| 100 mM | 0.0234 mL | 0.1170 mL | 0.2339 mL | 0.5848 mL |
NVP-BAG956 Related Classifications
HY-13333 Related Classifications
Powered by Bioz