BAY1082439
Based on 1 Customer Validation
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.
For research use only. We do not sell to patients.
- Purity: 99.35%
- CAS No.: 1375469-38-7
- Formula: C25H30N6O5
- Molecular Weight:494.54
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
|
PI3Kα |
PI3Kβ |
PI3Kδ |
BAY1082439 is a highly selective PI3Kα/α-balanced inhibitor. BAY1082439 has an IC50 ratio of 1:3 in biochemical assays of PI3Kα (4.9 nM) vs. PI3Kα (15.0 nM), and >1000-fold selectivity against mTOR kinase[1].
BAY1082439 (0.1-1 μM; 72 hours) is more effective than PI3Kα- and/or PI3Kβ-selective inhibitors in blocking PTEN-null prostate cancer cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3 and LNCaP cells (PTEN-null human prostate cancer cell lines)
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Concentration:0.1, 0.33, 1, 3.3, 10 μM
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Incubation Time:72 hours
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Result:Efectively inhibited cell growth by blocking the G1/S cell cycle transition and by inducing apoptosis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pten conditional knockout mouse model (Pb-Cre+;PtenL/L, CP model)[2]
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Dosage:75 mg/kg
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Administration:P.o.; daily for 4 weeks
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Result:Significantly decreased tumor size and P-AKT staining, nearly normal luminal architecture, and a significant reduction of Ki67-positive cells. Significantly inhibit the human prostate cancer growth.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1375469-38-7
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Appearance Solid
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Molecular Weight 494.54
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Formula C25H30N6O5
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Color White to off-white
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SMILES
O=C(C1=CC=CN=C1C)NC2=NC3=C(C=CC(OC[C@H](O)CN4CCOCC4)=C3OC)C5=NCCN25
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
0.1 M HCl : 16.67 mg/mL (33.71 mM; ultrasonic and warming and heat to 60°C)
DMSO : 5 mg/mL (10.11 mM; ultrasonic and adjust pH to 5 with HCl; 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)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 25 mg/mL (50.55 mM); Suspended solution; Need ultrasonic
Purity & Documentation
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Data Sheet (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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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 / 0.1 M HCl | 1 mM | 2.0221 mL | 10.1104 mL | 20.2208 mL | 50.5520 mL |
| 5 mM | 0.4044 mL | 2.0221 mL | 4.0442 mL | 10.1104 mL | |
| 10 mM | 0.2022 mL | 1.0110 mL | 2.0221 mL | 5.0552 mL | |
| 0.1 M HCl | 15 mM | 0.1348 mL | 0.6740 mL | 1.3481 mL | 3.3701 mL |
| 20 mM | 0.1011 mL | 0.5055 mL | 1.0110 mL | 2.5276 mL | |
| 25 mM | 0.0809 mL | 0.4044 mL | 0.8088 mL | 2.0221 mL | |
| 30 mM | 0.0674 mL | 0.3370 mL | 0.6740 mL | 1.6851 mL |
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