MLN1117

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MLN1117 (INK1117,TAK-117, Serabelisib) 是一种有效的选择性 PI3K p110α 抑制剂，IC50 为 15 nM。

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).

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.

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).

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

PI3K/Akt/mTOR signaling

PI3K

mTOR|p110α|p110β|p110γ|p110δ

Cancer

Breast Cancer

1268454-23-4

363.37

C19H17N5O3

>98% (HPLC)

DMSO: 6.4 mg/mL (Need ultrasonic or warming)

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

Methanone, [6-(2-amino-5-benzoxazolyl)imidazo[1,2-a]pyridin-3-yl]-4-morpholinyl-

(-20℃)

With Ice Pack

≥ 2 years