化合物 T16841 T16841

Product Introduction
Bioactivity


英文名: SAR-260301

描述: SAR-260301 is an orally available and selective inhibitor of PI3Kβ (IC50: 23 nM).

体外活性: SAR-260301 inhibits pAktS473 (a measured IC50: 0.06 μM and an estimated IC90: 2 μM), in the UACC-62 tumor cell line assay. SAR260301 inhibits PI3Kβ-dependent proliferation/viability in low serum conditions (IC50: 196 nM), in the MEF-3T3-myr-p110β mechanistic model. SAR260301 inhibits LNCaP cell proliferation in low and high serum conditions (IC50: 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). SAR260301 also leads to antitumor activities in PTEN-deficient/BRAF-mutant human melanoma cells, inhibiting cell proliferation (IC40: 6.5 and 3.3 μM for UACC-62 and WM-266.4, respectively, after 4-day treatment). 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 [2].

体内活性: SAR-260301 is well tolerated at the active dose, with no sign of toxicity and no bodyweight loss. 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(p.o.) reveals sustained target inhibition (≥50%) of pAkt-S473 for at least 7 h. SAR-260301 has moderate terminal elimination half-life (t1/2=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, p.o.), mice (100 mg/kg, p.o.), female nude rats (3 mg/kg, iv), rat (10 mg/kg, p.o.), male beagle dogs (10 mg/kg, p.o.)) [1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 125 mg/mL (352.71 mM)


关键字: SAR260301 | SAR 260301 | SAR-260301

相关产品: Protectin D1 | MOMIPP | iMDK | BGT226 | (+)-Nortrachelogenin | Dehydroglyasperin D | 7-(4-Hydroxyphenyl)-1-phenyl-4-hepten-3-one | GNE-490 | Jolkinolide B | ZSTK474

相关库: ReFRAME Related Library

化合物 T16841 T16841信息由TargetMol中国为您提供，如您想了解更多关于化合物 T16841 T16841报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途