Cat. No.: HY-12285

Serabelisib

Name: Serabelisib
Brand: MedChemExpress
SKU: HY-12285
Price: 70.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: MLN1117; INK1117; TAK-117)

Customer Review

Based on 1 Customer Validation

Serabelisib (MLN1117) is a selective p110α inhibitor with an IC₅₀ of 15 nM.

For research use only. We do not sell to patients.

Purity : 99.44%
CAS No.: 1268454-23-4
Formula: C₁₉H₁₇N₅O₃
Molecular Weight:363.37

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Serabelisib Chemical Structure

CAS No.: 1268454-23-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Protocols (1)
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Serabelisib (MLN1117) is a selective p110α inhibitor with an IC₅₀ of 15 nM.

IC₅₀ & Target

^[1]

p110α

15 nM (IC₅₀)

p110γ

1900 nM (IC₅₀)

p110β

4500 nM (IC₅₀)

p110δ

13900 nM (IC₅₀)

mTOR

1670 nM (IC₅₀)

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	14.11 μM Compound: 8a (TAK-117)	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	[PMID: 37651880]
HCT-116	IC₅₀	5.8 μM Compound: 8a (TAK-117)	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	[PMID: 37651880]
MCF-10A	IC₅₀	34.15 μM Compound: 8a (TAK-117)	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	[PMID: 37651880]
MCF7	IC₅₀	0.64 μM Compound: 8a (TAK-117)	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	[PMID: 37651880]
MCF7	IC₅₀	3.76 μM Compound: 8a (TAK-117)	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	[PMID: 37651880]
MDA-MB-231	IC₅₀	15.81 μM Compound: 8a (TAK-117)	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	[PMID: 37651880]
NCM460	IC₅₀	29.01 μM Compound: 8a (TAK-117)	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	[PMID: 37651880]
SW-620	IC₅₀	9.99 μM Compound: 8a (TAK-117)	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	[PMID: 37651880]

In Vitro

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. Further protocols information, click here.

In Vivo

Treatment with Serabelisib (MLN1117) at 30 and 60 mg/kg causes little reduction of TNP-specific IgG3. Notably, reduction of TNP-specific IgG3 at higher doses of Serabelisib (MLN1117) (120 mg/kg) is observed, consistent with the partial reduction in cell division in B cells treated with Serabelisib before anti-IgM stimulation. However, 120 mg/kg is above the effective dose of Serabelisib (MLN1117) for tumor growth inhibition (30-60 mg/kg)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1268454-23-4
Appearance Solid
Molecular Weight 363.37
Formula C₁₉H₁₇N₅O₃
Color White to gray
SMILES

O=C(C1=CN=C2C=CC(C3=CC=C(OC(N)=N4)C4=C3)=CN21)N5CCOCC5
Synonyms

MLN1117; INK1117; TAK-117
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7520 mL

13.7601 mL

27.5202 mL

5 mM

0.5504 mL

2.7520 mL

5.5040 mL

10 mM

0.2752 mL

1.3760 mL

2.7520 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. So L, et al. Selective inhibition of phosphoinositide 3-kinase p110α preserves lymphocyte function. J Biol Chem. 2013 Feb 22;288(8):5718-31. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Serabelisib

All PI3K Isoforms