SN32976
Based on 1 Customer Validation
SN32976 is a potent and selective class I PI3K and mTOR inhibitor with IC50s of 15.1 nM, 461 nM, 110 nM, 134 nM and 194 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively. SN32976 shows high selectivity among other 442 kinases. SN32976 shows anticancer effects.
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- Purity: 99.49%
- CAS No.: 1246202-11-8
- 화학식: C24H33F2N9O4S
- 분자량:581.64
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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PI3Kα 15.1 nM (IC50) |
PI3Kβ 461 nM (IC50) |
PI3Kγ 110 nM (IC50) |
PI3Kδ 134 nM (IC50) |
mTOR 194 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
206 nM
Compound: SN32976; 16
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Inhibition of recombinant human N-terminal p110delta/p85alpha expressed in baculovirus infected Sf9 insect cells using PIP2 as substrate by HTRF assay
Inhibition of recombinant human N-terminal p110delta/p85alpha expressed in baculovirus infected Sf9 insect cells using PIP2 as substrate by HTRF assay
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[PMID: 30850264] |
| Sf9 | IC50 |
5.3 nM
Compound: SN32976; 16
|
Inhibition of recombinant human N-terminal p110alpha/p85alpha expressed in baculovirus infected Sf9 insect cells using PIP2 as substrate by HTRF assay
Inhibition of recombinant human N-terminal p110alpha/p85alpha expressed in baculovirus infected Sf9 insect cells using PIP2 as substrate by HTRF assay
|
[PMID: 30850264] |
| Sf9 | IC50 |
743 nM
Compound: SN32976; 16
|
Inhibition of recombinant human N-terminal p110beta/p85alpha expressed in baculovirus infected Sf9 insect cells using PIP2 as substrate by HTRF assay
Inhibition of recombinant human N-terminal p110beta/p85alpha expressed in baculovirus infected Sf9 insect cells using PIP2 as substrate by HTRF assay
|
[PMID: 30850264] |
SN32976 (1-100 nM; for 1 h) inhibits both Thr308 and Ser473 pAKT expression in U-87 MG cells at concentrations as low as 10 nM[1].
The cell lines are PTEN null (U-87 MG, PC3, NZM34), H1047R PIK3CA mutant (HCT116, NZM40), E545K PIK3CA mutant (NCI-H460, MCF7) and PIK3CA amplified (FaDu). SN32976 potently inhibits cell proliferation in all cell lines, with EC50 values ranging from 18.5 nM in NCI-H460 cells to 1787 nM in NZM34 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U-87 MG cells
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Concentration:1 nM, 3 nM, 10 nM, 30 nM, 100 nM
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Incubation Time:for 1 h
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Result:Inhibited both Thr308 and Ser473 pAKT expression in U-87 MG cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-8 week old female balb/c nude or female balb/c Rag1−/− mice inoculated with U-87 MG cells[1]
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Dosage:37.5 mg/kg; 75 mg/kg
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Administration:po; daily; for 21 days
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Result:Inhibited tumor growth in U-87 MG tumor xenograft models.
Chemical Information
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CAS No. 1246202-11-8
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Appearance Solid
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분자량 581.64
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화학식 C24H33F2N9O4S
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Color Off-white to light yellow
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SMILES
O=S(CCN(C)C)(N1CCN(C2=NC(N3C4=CC=CC(OC)=C4N=C3C(F)F)=NC(N5CCOCC5)=N2)CC1)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 10 mg/mL (17.19 mM; ultrasonic and warming and heat to 60°C; 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
순도&문서
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 1 mM | 1.7193 mL | 8.5964 mL | 17.1928 mL | 42.9819 mL |
| 5 mM | 0.3439 mL | 1.7193 mL | 3.4386 mL | 8.5964 mL | |
| 10 mM | 0.1719 mL | 0.8596 mL | 1.7193 mL | 4.2982 mL | |
| 15 mM | 0.1146 mL | 0.5731 mL | 1.1462 mL | 2.8655 mL |