计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
SAR-260301 is an orally available and selective PI3Kβ inhibitor with an IC 50 of 23 nM
In Vitro
In the UACC-62 tumor cell line assay, SAR-260301 inhibits pAktS473 with a measured IC 50 at 0.06 μM and an estimated IC 90 at 2 μM. In MEF-3T3-myr-p110β mechanistic model, SAR260301 inhibits PI3Kβ-dependent proliferation/viability in low serum conditions with an IC 50 of 196 nM. In PTEN-deficient human prostate tumor cells, SAR260301 inhibits LNCaP cell proliferation in low and high serum conditions with IC 50 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 IC 40 values of 6.5 and 3.3 μM for UACC-62 and WM-266.4, respectively, after 4-day treatment. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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)) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
Cell proliferation is measured by quantifying intracellular ATP using CellTiter-Glo kit. Cells seeded into 96-well black microplates in complete medium, are treated with single or combined agents (e.g., SAR260301) 0.3 nM-30 μM (0.1% DMSO final concentration) for 96 hours. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:PI3Kβ 23 nM (IC 50 ) PI3Kδ 468 nM (IC 50 ) PI3Kα 1539 nM (IC 50 ) PI3Kγ 10000 nM (IC 50 ) Vps34 183 nM (IC 50 ) PI3KC2γ 3812 nM (IC 50 ) pAkt 49 nM (IC 50 ) DNA-PK 2000 nM (IC 50 )
规格
规格或纯度
10mM in DMSO
英文名称
SAR-260301
生化机理
SAR-260301 是一种可口服的选择性 PI3Kβ 抑制剂，其 IC 50 为 23 nM。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
C[C@H]1CC2=CC=CC=C2N1C(=O)CC3=NC(=CC(=O)N3)N4CCOCC4
PubChem CID
分子量
354.40
技术文档
高级数据
关联靶点（人）
PIK3CB
Tchem
磷脂酰肌醇 4,5-双磷酸 3-激酶催化亚基 β 异构体(Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform)
(0 活性数据)
AKT1
Tchem
RAC-alpha 丝氨酸/苏氨酸蛋白激酶(RAC-alpha serine/threonine-protein kinase)
(0 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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