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SAR-260301

CAS No. : 1260612-13-2

MCE 站：SAR-260301

产品活性：SAR-260301 是一种有效的，具有口服活性的选择性 PI3Kβ 抑制剂，IC₅₀ 为 23 nM。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K

In Vitro: In the UACC-62 tumor cell line assay, SAR-260301 inhibits pAktS473 with a measured IC₅₀ at 0.06 μM ａnd an estimated IC₉₀ at 2 μM. In MEF-3T3-myr-p110β mechanistic model, SAR260301 inhibits PI3Kβ-dependent proliferation/viability in low serum conditions with an IC₅₀ of 196 nM. In PTEN-deficient human prostate tumor cells, SAR260301 inhibits LNCaP cell proliferation in low ａnd high serum conditions with IC₅₀ values of 2.9 ａnd 5.0 μM, respectively, after 4-day treatment, whereas it is inactive in these conditions in PC3 cells at concentrations up to 10 μM, despite target engagement. After prolonged treatment, SAR260301 at 3 or 10 μM inhibits PC3 cell proliferation in low serum conditions, with a cytostatic effect achieved for 14 days, despite some cell death induction observed at 10 μM. SAR260301 also leads to antitumor activities in PTEN-deficient/BRAF-mutant human melanoma cells, inhibiting cell proliferation with IC₄₀ values of 6.5 ａnd 3.3 μM for UACC-62 ａnd WM-266.4, respectively, after 4-day treatment.

In Vivo: SAR-260301 displays antitumor efficacy in human PTEN-deficient melanoma models in mice as a single agent. SAR-260301 treatment leads to a statistically significant tumor growth inhibition as measured by a ΔT/ΔC of 39% (p = 0.054 versus control mice) on day 15 post-tumor implantation. SAR-260301 is well tolerated at the active dose, with no sign of toxicity ａnd no body weight loss. Oral administration of SAR-260301 reveals sustained target inhibition (≥50%) of pAkt-S473 for at least 7 h. SAR-260301 has moderate terminal elimination half-life (t_1/2=0.87 h, 1.4 h, 2.5 h, 0.87h, 6.9 h ａnd 4.5 h for female SCID mice (3 mg/kg, iv), mice (10 mg/kg, po), mice (100 mg/kg, po), female nude rats (3 mg/kg, iv), rat (10 mg/kg, po), male beagle dogs (10 mg/kg, po)).

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