MLN1117 - CAS 1268454-23-4
Catalog number: 1268454-23-4
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
MLN1117, also known as INK1117, is a PI3Kα inhibitor which could lead to the apoptosis and growth retardation of tumor cells expressed by PI3Kα. IC50: 15 nM.
INK1117; INK-1117; INK 1117; MLN1117; MLN 1117; MLN-1117; TAK-117; TAK 117; TAK117; Serabelisib; [6-(2-amino-1,3-benzoxazol-5-yl)imidazo[1,2-a]pyridin-3-yl]-morpholin-4-ylmethanone;Serabelisib
DMSO: ≥ 6.4 mg/mL (Need ultrasonic or warming)
-20ºC Freeze
MLN1117 is a PI3Kα inhibitor which could lead to the apoptosis and growth retardation of tumor cells expressed by PI3Kα.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Canonical SMILES:
1.Co-targeting aurora kinase with PD-L1 and PI3K abrogates immune checkpoint mediated proliferation in peripheral T-cell lymphoma: a novel therapeutic strategy.
Islam S;Vick E;Huber B;Morales C;Spier C;Cooke L;Weterings E;Mahadevan D Oncotarget. 2017 Nov 1;8(59):100326-100338. doi: 10.18632/oncotarget.22222. eCollection 2017 Nov 21.
Peripheral T-cell non-Hodgkin lymphoma (PTCL) are heterogeneous, rare, and aggressive diseases mostly incurable with current cell cycle therapies. Aurora kinases (AKs) are key regulators of mitosis that drive PTCL proliferation. Alisertib (AK inhibitor) has a response rate ∼30% in relapsed and refractory PTCL (SWOG1108). Since PTCL are derived from CD4;+;/CD8;+; cells, we hypothesized that Program Death Ligand-1 (PD-L1) expression is essential for uncontrolled proliferation. Combination of alisertib with PI3Kα (MLN1117) or pan-PI3K inhibition (PF-04691502) or vincristine (VCR) was highly synergistic in PTCL cells. Expression of PD-L1 relative to PD-1 is high in PTCL biopsies (∼9-fold higher) and cell lines. Combination of alisertib with pan-PI3K inhibition or VCR significantly reduced PD-L1, NF-κB expression and inhibited phosphorylation of AKT, ERK1/2 and AK with enhanced apoptosis. In a SCID PTCL xenograft mouse model, alisertib displayed high synergism with MLN1117. In a syngeneic PTCL mouse xenograft model alisertib demonstrated tumor growth inhibition (TGI) ∼30%, whilst anti-PD-L1 therapy alone was ineffective. Alisertib + anti-PD-L1 resulted in TGI >90% indicative of a synthetic lethal interaction.
2.A First-in-Human, Phase I, Dose-Escalation Study of TAK-117, a Selective PI3Kα Isoform Inhibitor, in Patients with Advanced Solid Malignancies.
Juric D;de Bono JS;LoRusso PM;Nemunaitis J;Heath EI;Kwak EL;Macarulla Mercadé T;Geuna E;Jose de Miguel-Luken M;Patel C;Kuida K;Sankoh S;Westin EH;Zohren F;Shou Y;Tabernero J Clin Cancer Res. 2017 Sep 1;23(17):5015-5023. doi: 10.1158/1078-0432.CCR-16-2888. Epub 2017 May 10.
Purpose:; To evaluate the safety, MTD, pharmacokinetics, pharmacodynamics, and preliminary antitumor activity of TAK-117 (MLN1117/INK1117), an investigational PI3Kα-selective inhibitor, in patients with advanced solid tumors.;Experimental Design:; Seventy-one patients received oral TAK-117 once daily [100-300 mg (;n; = 24)] or 3 days per week [Monday-Wednesday-Friday (MWF), 200-1,200 mg (;n; = 27); Monday-Tuesday-Wednesday (MTuW), 200-900 mg (;n; = 20)], in 21-day cycles. Dose escalation proceeded via a 3 + 3 design.;Results:; TAK-117 once-daily dosing was associated with dose-limiting grade ≥3 alanine/aspartate aminotransferase (ALT/AST) elevations, resulting in a narrow range of tolerable doses (100-150 mg once daily). With MWF/MTuW dosing, no dose-limiting ALT/AST elevations occurred until the MTD of 900 mg; total weekly dose was 2.6-fold that of 150 mg once daily. Drug-related grade ≥3 adverse events occurred in 25%/22%/35% (including hyperglycemia in 0%/7%/15%) of once-daily/MWF/MTuW patients. TAK-117 (100-1,200 mg) exhibited moderately fast oral absorption, a generally dose proportional increase in exposure, and plasma half-life of approximately 11 hours. Total weekly exposures with 900 mg MWF/MTuW dosing were approximately 4 times greater than with 150 mg once daily.
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