| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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Purity: ≥98%
NVP-BAG956 (also known as BAG-956) is a novel, potent and ATP-competitive PI3K inhibitor with anticancer activity. It inhibits PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ with IC50 values of 34, 56, 112 and 444 nM, respectively. NVP-BAG956 is also a PDK1 inhibitor, and has been shown to inhibit cellular AKT phosphorylation at Thr308. BAG 956 also blocks cell proliferation and causes arrest in the G1 phase of the cell cycle. BAG 956 has been shown to slow tumor progression in mouse xenograft models.
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| ln Vitro |
NVP-BAG956 has an IC50 of 240/260 nM and inhibits PDK1 as well. VEGFR1 is likewise inhibited by NVP-BAG956, with an IC50 of 2.56±0.56 μM.nM. NVP-BAG956 (IC50=290±20 nM)-induced inhibition of PKB/Akt phosphorylation was associated with decreased A2058 cell proliferation. NVP-BAG956 causes A2058 cells to only be able to exit G2-M and stay in G1. NVP-BAG956 clearly induces the expression of p27 Kip1 in A2058 cells, but not in C32 cells[1].
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| Cell Assay |
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| References |
| Molecular Formula |
C28H21N5
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|---|---|
| Molecular Weight |
427.49984
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| Exact Mass |
427.179
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| CAS # |
853910-02-8
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| PubChem CID |
24882589
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
694.8±65.0 °C at 760 mmHg
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| Flash Point |
374.0±34.3 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.655
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| LogP |
4.75
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
33
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| Complexity |
806
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HSQAARMBHJCUOK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H35ClN2O2/c25-22-5-4-17(3-1-6-26-7-2-8-28)12-21(22)23(29)27-16-24-13-18-9-19(14-24)11-20(10-18)15-24/h4-5,12,18-20,26,28H,1-3,6-11,13-16H2,(H,27,29)
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| Chemical Name |
Benzamide, 2-chloro-5-(3-((3-hydroxypropyl)amino)propyl)-N-(tricyclo(3.3.1.13,7)dec-1-ylmethyl)-
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| Synonyms |
NVP-BAG956; BAG-956; NVP-BAG-956; BAG 956; NVP-BAG 956; BAG956;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~116.96 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.85 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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