Serabelisib
Based on 1 Customer Validation
Serabelisib (MLN1117) is a selective p110α inhibitor with an IC50 of 15 nM.
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- Pureté: 99.44%
- CAS No.: 1268454-23-4
- Formule: C19H17N5O3
- Masse moléculaire:363.37
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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p110α 15 nM (IC50) |
p110γ 1900 nM (IC50) |
p110β 4500 nM (IC50) |
p110δ 13900 nM (IC50) |
mTOR 1670 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
14.11 μM
Compound: 8a (TAK-117)
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Antiproliferative activity against human HCT-116 cells expressing PIK3CA with H1047R mutation assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
Antiproliferative activity against human HCT-116 cells expressing PIK3CA with H1047R mutation assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
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[PMID: 37651880] |
| HCT-116 | IC50 |
5.8 μM
Compound: 8a (TAK-117)
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Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
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[PMID: 37651880] |
| MCF-10A | IC50 |
34.15 μM
Compound: 8a (TAK-117)
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Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
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[PMID: 37651880] |
| MCF7 | IC50 |
0.64 μM
Compound: 8a (TAK-117)
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Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
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[PMID: 37651880] |
| MCF7 | IC50 |
3.76 μM
Compound: 8a (TAK-117)
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Antiproliferative activity against human MCF7 cells expressing PIK3CA with E545K mutation assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells expressing PIK3CA with E545K mutation assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
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[PMID: 37651880] |
| MDA-MB-231 | IC50 |
15.81 μM
Compound: 8a (TAK-117)
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Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
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[PMID: 37651880] |
| NCM460 | IC50 |
29.01 μM
Compound: 8a (TAK-117)
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Cytotoxicity against human NCM460 cells assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
Cytotoxicity against human NCM460 cells assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
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[PMID: 37651880] |
| SW-620 | IC50 |
9.99 μM
Compound: 8a (TAK-117)
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Antiproliferative activity against human SW-620 cells assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
Antiproliferative activity against human SW-620 cells assessed as reduction in cell viability incubated for 24 to 48 hrs by CCK-8 assay
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[PMID: 37651880] |
Serabelisib (MLN1117) inhibits Akt phosphorylation and growth in PIK3CA mutant breast cancer cells with IC50s around 2 μM, yet has no effect on cells lacking PTEN. BCR-stimulated B cells treated with 1 μM Serabelisib (MLN1117) displays a significant reduction (up to 50%) in the magnitude of the phosphorylated Akt (p-Akt) signal measured by intracellular flow cytometry. The effect of Serabelisib is dose-dependent[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1268454-23-4
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Appearance Solid
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Masse moléculaire 363.37
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Formule C19H17N5O3
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Color White to gray
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SMILES
O=C(C1=CN=C2C=CC(C3=CC=C(OC(N)=N4)C4=C3)=CN21)N5CCOCC5
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Synonyms
MLN1117; INK1117; TAK-117
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
DMSO : 6.4 mg/mL (17.61 mM; Need ultrasonic and warming; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
A total of 5000 SK-OV-3 and U87MG cell lines/well in low serum media (0.2% FBS) are seeded in triplicate wells of a 96-well flat bottom culture plate for 18 h to adhere. Media is aspirated and inhibitors in 0.2% FBS media are added to each well at the indicated concentrations. After 48 h, cell viability is determined using the MTS assay (Cell Titer 96 Aqueous One solution cell proliferation assay kit) with absorbance (490 nm) measured in a microplate spectrophotometer[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Wild-type 8-week-old Balb/cJ mice are used for all experiments. Serabelisib and GDC-0941 are given by oral gavage using a sterile disposable 20-guage 1.5′ feeding needle. IC87114 is delivered via intraperitoneal injection. For the non-immunization experiment, 2 mice per group (Vehicle, GDC-0941, and Serabelisib (MLN1117)) are given the indicated drugs for 9 days before sacrificing on day 10. For the immunization experiment, 4 mice per group are used to perform two independent studies comparing GDC-0941 or IC87114 to Serabelisib (MLN1117). In all cases, the vehicle group receive both vehicles used to formulate the two different drugs. Mice are treated with the drugs throughout day -1 to day 13. On day 0, all mice are immunized with NP-OVA precipitated in alum. Drug treatment is stopped on day 13 and mice are sacrificed for collection of serum and spleens.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7520 mL | 13.7601 mL | 27.5202 mL | 68.8004 mL |
| 5 mM | 0.5504 mL | 2.7520 mL | 5.5040 mL | 13.7601 mL | |
| 10 mM | 0.2752 mL | 1.3760 mL | 2.7520 mL | 6.8800 mL | |
| 15 mM | 0.1835 mL | 0.9173 mL | 1.8347 mL | 4.5867 mL |
Serabelisib Related Classifications
HY-12285 Related Classifications
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