计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，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
2-8°C储存。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
S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl . S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis , increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC , LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3 , TIE2, KIT, PDGFR-β. Antitumor activies
In Vitro
S116836 (0.01-1 μM; 24 hours) significantly reduces the cellular proliferation of BaF3/WT and BaF3/T315I cells (IC 50 values of 0.05 μM and 0.20 μM, respectively). S116836 (0.01-1 μM; 24 hours) significantly downregulates the expression level of p-BCR-ABL in BaF3/WT cells. S116836 (0.01-1 μM; 24 hours) also significantly downregulates the expression level of p-Crkl and p-STAT5 (downstream signaling proteins of BCR-ABL) in both BaF3/WT and BaF3/T315I cells. S116836 (0.1, 0.3, and 0.5 μM; 24 hours) arrests the BaF3/WT and BaF3/T315I cells in G0/G1 phase of the cell cycle. S116836 (0.3 and 0.5 μM; 24 hours) increases ROS production and decreases GSH levels in BaF3/WT and BaF3/T315I cells. S116836 (0.1, 0.3, and 0.5 μM; 24 hours) induces apoptosis in BaF3/WT and BaF3/T315I cells. S116836 potently inhibits PDGFRα and its downstream signaling molecules such as STAT3, AKT, and Erk1/2. S116836 effectively inhibits the growth of the WT and T674I FIP1L1-PDGFRα-expressing neoplastic cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
S116836 (100 or 200 mg/kg; i.p.; q3d×6, athymic NCR nude mice) decreases the volume and weight of xenograft tumors expressing WT and T315I mutant BCR-ABL . S116836 (200mg/kg/d, oral gavage for 14 days) inhibits the growth of xenografted T674I-FIP1L1-PDGFRα cells in nude mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:Bcr-Abl WT Bcr-Abl T315I
规格
规格或纯度
≥99%
英文名称
S116836
生化机理
S116836是一种强效的口服活性BCR-ABL酪氨酸激酶抑制剂，可阻断野生型和T315I Bcr-Abl。S116836 可使细胞停滞在细胞周期的 G0/G1 期，诱导细胞凋亡，增加 ROS 的产生，并减少细胞内 GSH 的产生。
储存条件
2-8°C储存
运输条件
低温运输
纯度
≥99%
名称和识别符
分子类型
小分子
Smiles
O=C(C1=CC=C(C(C#CC2=CN=C(N=C2)NC3CC3)=C1)C)NC4=CC(C(F)(F)F)=CC(N5C=CN=C5)=C4
分子量
502.49
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 32 mg/mL (63.68 mM; ultrasonic and warming and heat to 80°C)
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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