MLN1117

SKU: orb1226634

Description

MLN1117 (INK1117,TAK-117, Serabelisib) is a potent, selective PI3K p110α inhibitor with IC50 of 15 nM, displays >300-fold selectivity over p110β/γ/δ and mTOR; inhibits AKT phosphorylation and growth in PIK3CA mutant breast cancer cells with IC50 of 2 uM, significantly suppresses B cell proliferation driven by anti-IgM alone but not by anti-IgM plus IL-4; abrogates immune checkpoint mediated proliferation in peripheral T-cell lymphoma combined with alisertib.Breast Cancer Phase 2 Clinical(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).

Key Properties

• CAS Number: 1268454-23-4
• MW: 363.37
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₇N₅O₃
• SMILES: O=C(C1=CN=C2C=CC(C3=CC=C(OC(N)=N4)C4=C3)=CN21)N5CCOCC5
• Target: PI3K
• Solubility: DMSO: 6.4 mg/mL (Need ultrasonic or warming)

Bioactivity

• 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).
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

INK1117 | TAK-117 | TAK117 | Serabelisib | INK 1117

Quick Database Links

Gene Symbol

PI3K