1. PI3K/Akt/mTOR
  2. PI3K

Serabelisib (Synonyms: MLN1117; INK1117)

Cat. No.: HY-12285 Purity: 99.66%
Handling Instructions

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
25 mg USD 288 In-stock
Estimated Time of Arrival: December 31
50 mg USD 420 In-stock
Estimated Time of Arrival: December 31
100 mg USD 660 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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 ${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].

In Vivo

Treatment with Serabelisib at 30 and 60 mg/kg causes little reduction of TNP-specific IgG3. Notably, reduction of TNP-specific IgG3 at higher doses of Serabelisib (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 for tumor growth inhibition (30-60 mg/kg)[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 6.4 mg/mL (17.61 mM; Need ultrasonic and warming)

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
10 mM 0.2752 mL 1.3760 mL 2.7520 mL
*Please refer to the solubility information to select the appropriate solvent.
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) 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. 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
Molecular Weight

363.37

Formula

C₁₉H₁₇N₅O₃

CAS No.

1268454-23-4

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.66%

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Product Name:
Serabelisib
Cat. No.:
HY-12285
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Serabelisib

Cat. No.: HY-12285