Description
Serabelisib (MLN1117) is a selective p110α inhibitor with an IC50 of 15 nM.
Product information
CAS Number: 1268454-23-4
Molecular Weight: 363.37
Formula: C19H17N5O3
Chemical Name: 5-[3-(morpholine-4-carbonyl)imidazo[1,2-a]pyridin-6-yl]-1,3-benzoxazol-2-amine
Smiles: NC1=NC2=CC(=CC=C2O1)C1=CN2C(=CN=C2C=C1)C(=O)N1CCOCC1
InChiKey: BLGWHBSBBJNKJO-UHFFFAOYSA-N
InChi: InChI=1S/C19H17N5O3/c20-19-22-14-9-12(1-3-16(14)27-19)13-2-4-17-21-10-15(24(17)11-13)18(25)23-5-7-26-8-6-23/h1-4,9-11H,5-8H2,(H2,20,22)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 6.4 mg/mL (17.61 mM; Need ultrasonic and warming).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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).
Products are for research use only. Not for human use.
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