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) |
|---|
TG100-115, PI3 激酶 p110-delta 亚基抑制剂
有货
为什么选择此级别
Moligand™ 级 ，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
TG100-115是PI3K γ和δ抑制剂，IC50分别为83和235 nM。A PI3K and FRAP inhibitor with some action against Akt
Information
TG100-115 is aPI3Kγ/δinhibitor withIC50of 83 nM/235 nM, with little effect on PI3Kα/β. Phase 1/2.
In vitro
TG100-115 inhibits PI3Kγ and -δ, with IC50 of 83 and 235 nM, respectively. TG100-115 is not active for PI3Kα and -β, with IC50 of 1.2 and 1.3 mM. In human umbilical vein endothelial cells (HUVECs), TG100-115 (up to 10 μM) has no effects on cell proliferation and VEGF-stimulated ERK phosphorylation. However, TG100-115 (10 μM) interrupts other VEGF signaling pathways, such as those that culminate in VE-cadherin phosphorylation. In HUVECs, TG100-115 (10 μM) inhibits the VEGF-induced increase of total level of VE-cadherin. TG100-115 inhibits VEGF mediated phosphorylation of mTOR and p70S6 kinase, both of which are downstream of PI3K. TG100-115 (125 nM to 10 μM) also inhibits FGF-stimulated phosphorylation of Akt.
In vivo
In Miles assay models, TG100-115 (1-5 mg/kg) reduces edema formation and inflammation in rats. In rigorous rodent and porcine models of myocardial ischemia (MI), TG100-115 (0.5-5 mg/kg) provides potent cardioprotection, limits infarct development, and preserves myocardial function. In mice, TG100-115 (5 mg/kg) markedly diminishes vascular permeability (VP) in response to either Sema3A or VEGF, indicating that both factors may depend on PI3Kγ/δ to induce VP. In a mouse asthma model, aerosolized TG100-115 markedly reduces the pulmonary eosinophilia, inhibits interleukin-13 and mucin accumulation.
Cell Data
cell lines：
Concentrations：10 μM, dissolved in DMSO as stock solution
Incubation Time：24, 48, and 72 hours
Powder Purity:≥99%
规格
英文别名
6,7-Bis(3-hydroxyphenyl)pteridine-2,4-diamine
规格或纯度
Moligand™, 10mM in DMSO
英文名称
TG100-115
生化机理
TG100-115 是一种 PI3Kγ/δ 抑制剂，IC50 为 83 nM/235 nM，对 PI3Kα/β 几乎没有影响。1/2阶段。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
PI3 激酶 p110-delta 亚基抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1=CC(=CC(=C1)O)C2=NC3=C(N=C(N=C3N=C2C4=CC(=CC=C4)O)N)N
PubChem CID
分子量
346.35
技术文档
高级数据
产品属性
| ALogP | 1.7 |
|---|
关联靶点（人）
DCK
Tchem
脱氧胞苷激酶(Deoxycytidine kinase)
(1 活性数据)
TRPM6
Tchem
瞬时受体电位阳离子通道亚家族M成员6(Transient receptor potential cation channel subfamily M member 6)
(1 活性数据)
PIK3CG
Tclin
磷脂酰肌醇 4,5-双磷酸 3-激酶催化亚基 γ 异构体(Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform)
(2 活性数据)
PIK3CA
Tclin
磷脂酰肌醇 4,5-双磷酸 3-激酶催化亚基 α 异构体(Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform)
(1 活性数据)
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)
(1 活性数据)
PIK3CD
Tclin
磷脂酰肌醇 4,5-双磷酸 3-激酶催化亚基 delta 异构体(Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform)
(1 活性数据)
PIK3C2B
Tchem
磷脂酰肌醇 4-磷酸 3-激酶 C2 结构域亚基 β(Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta)
(1 活性数据)
PIK3C2G
Tchem
磷脂酰肌醇 4-磷酸 3-激酶 C2 结构域亚基 γ(Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 92 mg/mL (199.37 mM); Water: Insoluble; Ethanol: Insoluble;
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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