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Bimiralisib
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Catalog No. T2265Cas No. 1225037-39-7
Alias PQR309, PI3K-IN-2, 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine
Bimiralisib (PI3K-IN-2) is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.
Bimiralisib
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Purity: 98.92%
Catalog No. T2265Alias PQR309, PI3K-IN-2, 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amineCas No. 1225037-39-7
Bimiralisib (PI3K-IN-2) is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $30 | In Stock | In Stock | |
| 5 mg | $73 | In Stock | In Stock | |
| 10 mg | $118 | In Stock | In Stock | |
| 25 mg | $232 | In Stock | In Stock | |
| 50 mg | $378 | In Stock | In Stock | |
| 100 mg | $579 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $80 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:98.92%
Color:White to Yellow
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Product Introduction
Bimiralisib AI Summary
Bimiralisib demonstrates significant bioactivity across various biological assays. It exhibits potent antitumor activity against human PC3 and OVCAR-3 cell lines xenografted in rat and BALB/c nude mice models, with observable tumor reduction at multiple dosage levels, including 50 mg/kg and 6.3 mg/kg when administered orally. Additionally, the compound shows strong inhibition of pivotal kinases such as PI3K alpha, beta, delta, and gamma, as well as mTORC1 and mTORC2, with IC50 values ranging between 33.0 nM to over 700 nM, and Ki values of 17.0 nM and 62.0 nM against PI3Kalpha and mTOR, respectively. In antiviral assays, Bimiralisib effectively inhibits SARS-CoV-2-induced cytotoxicity in Caco-2 and VERO-6 cells, with notable inhibition rates at 10 µM concentration. The compound also displays metabolic stability across various species in liver microsomes, oral bioavailability, and efficient clearance in animal models. Furthermore, it shows inhibitory activity against HDAC6 enzyme in enzymatic assays and demonstrates selectivity towards PI3K signaling pathways, making it a promising candidate for therapeutic applications in oncology and virology..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Bimiralisib (PI3K-IN-2) is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy. |
| Targets&IC50 | PI3Kβ:11 nM(Kd), DNA-PK:8567 nM, PI3Kα:1.5 nM(Kd), PI3Kδ:25 nM(Kd), VPS34:6486 nM, PI3Kα (H1047R):36 nM, PI3Kα (E542K):136 nM, PI3Kα (E542K):63 nM, PI3Kγ:25 nM(Kd), mTOR:12 nM(Kd) |
| Synonyms | PQR309, PI3K-IN-2, 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine |
| Molecular Weight | 411.38 |
| Formula | C17H20F3N7O2 |
| Cas No. | 1225037-39-7 |
| Smiles | Nc1cc(c(cn1)-c1nc(nc(n1)N1CCOCC1)N1CCOCC1)C(F)(F)F |
| Relative Density. | 1.418 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 5 mg/mL (12.15 mM), Sonication is recommended.  | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.43 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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