byl719  (MedChemExpress)

Journal: bioRxiv

Article Title: Targeting PI3Kβ-dependent cancer with a novel small molecule inhibitor, GT220

doi: 10.64898/2026.01.16.699992

Figure Lengend Snippet: (A) Quantification of AKT phosphorylation at Thr308 and Ser473 in PTEN-null HCC70 cells following 1-hour treatment with GT220 or the indicated PI3K inhibitors (0.5 μM). Phospho-AKT levels are expressed as a percentage of control (mean ± SD). Statistical significance is indicated (P < 0.05; ****P < 0.0001). (B-C) Immunoblot analysis of AKT signaling in HCC70 (PTEN-null; B ) and HCC1954 (PTEN wild-type; C ) cells treated for 1 hour with increasing concentrations of GT220, KIN193 (PI3Kβ-selective), AZD8186 (PI3Kβ/δ), GSK2636771 (PI3Kβ-selective), or BYL719 (PI3Kα-selective). Phosphorylation of AKT at Thr308 and Ser473, total AKT, and vinculin (loading control) are shown. (D-E) Cell viability dose–response curves for HCC70 ( D ) and HCC1954 ( E ) cells treated for 72 hours with increasing concentrations of GT220 or comparator PI3K inhibitors. Cell viability is expressed relative to vehicle-treated controls (mean ± SD). Tables summarize IC₅₀ values (µM) derived from nonlinear regression analysis.

Article Snippet: KIN193, AZD8186, GSK2636771, BYL719 were purchased from MedChemExpress.

Techniques: Phospho-proteomics, Control, Western Blot, Derivative Assay

Journal: bioRxiv

Article Title: Targeting PI3Kβ-dependent cancer with a novel small molecule inhibitor, GT220

doi: 10.64898/2026.01.16.699992

Figure Lengend Snippet: (A) Quantification of AKT phosphorylation at Thr308 and Ser473 in PTEN-null HCC70 cells following 1-hour treatment with GT220 or the indicated PI3K inhibitors (0.5 μM). Phospho-AKT levels are expressed as a percentage of control (mean ± SD). Statistical significance is indicated (P < 0.05; ****P < 0.0001). (B-C) Immunoblot analysis of AKT signaling in HCC70 (PTEN-null; B ) and HCC1954 (PTEN wild-type; C ) cells treated for 1 hour with increasing concentrations of GT220, KIN193 (PI3Kβ-selective), AZD8186 (PI3Kβ/δ), GSK2636771 (PI3Kβ-selective), or BYL719 (PI3Kα-selective). Phosphorylation of AKT at Thr308 and Ser473, total AKT, and vinculin (loading control) are shown. (D-E) Cell viability dose–response curves for HCC70 ( D ) and HCC1954 ( E ) cells treated for 72 hours with increasing concentrations of GT220 or comparator PI3K inhibitors. Cell viability is expressed relative to vehicle-treated controls (mean ± SD). Tables summarize IC₅₀ values (µM) derived from nonlinear regression analysis.

Article Snippet: KIN193, AZD8186, GSK2636771, BYL719 were purchased from MedChemExpress.

Techniques: Phospho-proteomics, Control, Western Blot, Derivative Assay

Journal: bioRxiv

Article Title: Targeting PI3Kβ-dependent cancer with a novel small molecule inhibitor, GT220

doi: 10.64898/2026.01.16.699992

Figure Lengend Snippet: BALB/c nude mice bearing HCC70 xenografts were treated with GT220, KIN193, or AZD8186 at doses of 30, 60, or 90 mg/kg, administered orally twice daily (po, bid; n = 6 per group) for 3 days. Tumors and plasma were collected 1.5 hours after the final dose. (A–C) Tumor lysates were analyzed by immunoblotting for phosphorylated AKT (p-AKT) levels using the indicated antibodies. (D) Intratumoral drug concentrations measured by LC–MS/MS at the indicated doses for each compound. (E) Corresponding plasma drug concentrations measured by LC–MS/MS. Data in (D) and (E) are presented as mean ± SEM, with individual data points shown.

Article Snippet: KIN193, AZD8186, GSK2636771, BYL719 were purchased from MedChemExpress.

Techniques: Clinical Proteomics, Western Blot, Liquid Chromatography with Mass Spectroscopy

Journal: bioRxiv

Article Title: Targeting PI3Kβ-dependent cancer with a novel small molecule inhibitor, GT220

doi: 10.64898/2026.01.16.699992

Figure Lengend Snippet: BALB/c nude mice bearing established HCC70 (PTEN-deficient) xenografts were treated orally twice daily (po, bid; n = 6 per group) with GT220 ( A, B ), KIN193 ( C. D ), or AZD8186 ( E, F ) at doses of 30, 60, or 90 mg/kg for 21 days. Tumor volumes ( A, C, E ) and body weights (B, D, F) were measured every 2–3 days throughout the treatment period. ( G, H ) Antitumor efficacy and tolerability of the salt form GT220F administered orally twice daily at 10, 30, or 100 mg/kg (n = 6 per group) for 21 days. Tumor volumes ( G ) and body weights (H ) were monitored longitudinally. Data are presented as mean ± SEM. Statistical significance is indicated as shown (P < 0.05, *P < 0.01, **P < 0.005, ***P < 0.0001; one-way ANOVA). “ns” denotes not significant.

Article Snippet: KIN193, AZD8186, GSK2636771, BYL719 were purchased from MedChemExpress.

Techniques: