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  3. PI3K
  4. Serabelisib

Serabelisib  (Synonyms: MLN1117; INK1117; TAK-117)

Cat. No.: HY-12285 Purity: 99.21%
COA Handling Instructions

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

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

Serabelisib Chemical Structure

Serabelisib Chemical Structure

CAS No. : 1268454-23-4

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Serabelisib Related Antibodies

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Description

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

IC50 & Target

p110α

15 nM (IC50)

p110γ

1900 nM (IC50)

p110β

4500 nM (IC50)

p110δ

13900 nM (IC50)

mTOR

1670 nM (IC50)

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.

Serabelisib Related Antibodies
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
Molecular Weight

363.37

Formula

C19H17N5O3
CAS No.
Appearance

Solid

Color

White to gray

SMILES

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7520 mL 13.7601 mL 27.5202 mL
5 mM 0.5504 mL 2.7520 mL 5.5040 mL
View the 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.

  • Molarity Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.21%

COA (247 KB) LCMS (268 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Serabelisib1268454-23-4MLN1117 INK1117 TAK-117MLN 1117MLN-1117INK1117INK 1117INK-1117TAK117TAK 117TAK-117PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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