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
-20°C储存。超低温运输 。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
XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC 50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects
In Vitro
XST-14 inhibits ULK1 (IC 50 =13.6 nM), MAP2K1/MEK1 (IC 50 =721.8 nM), MAPK14/p38 alpha (IC 50 =283.9 nM), TGFBR2 (IC 50 =809.3 nM), ACVR1/ALK2 (IC 50 =183.8 nM), ULK2 (IC 50 =70.9 nM) and CAMK2A (IC 50 =66.3 nM) by the 10-point titration results from SelectScreen Kinase Profiling Services. XST-14 (20-80 μM; for 24 h) leads a decrease in cell proliferation activity. XST-14 (5 μM; for 24 h) induces apoptosis in HepG2 and human primary HCC cells. XST-14 (5 μM; for 12 h) strongly inhibits the conversion of LC3-I to LC3-II in CHO cells stably expressing GFP-LC3. XST-14 (5 μM; for 12 h) inhibits the Ser249 phosphorylation of PIK3C3 and Ser15 phosphorylation of BECN1. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: HepG2 cells Concentration: 20, 40, 60, 80 μM Incubation Time: 24 hours Result: Led a decrease in cell proliferation activity. Apoptosis AnalysisCell Line: HepG2 and human primary cells Concentration: 5 μM Incubation Time: 24 hours Result: Induced apoptosis in HepG2 and human primary HCC cells. Cell Autophagy AssayCell Line: CHO, HepG2 cells stably expressing GFP-LC3 Concentration: 5 μM Incubation Time: 12 hours Result: Strongly inhibited the conversion of LC3-I to LC3-II in CHO cells. Dramatically decreased the number of GFP-LC3 puncta in HepG2 cells. Decreased autophagosome formation and blocked autophagosome/lysosome fusion in HepG2 cells. Western Blot AnalysisCell Line: HepG2 cells Concentration: 5 μM Incubation Time: 12 hours Result: Inhibited the Ser249 phosphorylation of PIK3C3 and Ser15 phosphorylation of BECN1.
In Vivo
XST-14 (15, 30 mg/kg/day; IP; for 4 consecutive weeks) displays anti-HCC efficacies, resulting in decreased tumor weights and suppressed tumor growth of HCC cells in nude mice . XST-14 (2 mg/kg for IV; 10 mg/kg for IP) has a T 1/2 of 2.31 hours for IV and a T 1/2 of 2.69 hours for IP . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice bearing HepG2 tumor xenografts Dosage: 15, 30 mg/kg Administration: IP; daily; for 4 consecutive weeks Result: Displayed anti-HCC efficacies, resulting in decreased tumor weights and suppressed tumor growth of HCC cells in nude mice. Animal Model: Sprague-Dawley rat Dosage: 2 mg/kg for IV; 10 mg/kg for IP (Pharmacokinetic Analysis) Administration: IV or IP Result: Had a T 1/2 of 2.31 hours, a CL of 26.28 mL/min•kg, and and an AUC of 1269 hr•ng/mL for IV. Had a T 1/2 of 2.69 hours, a C max of 2033 ng/mL, and an AUC of 5979 hr•ng/mL for IP.
Form:Solid
IC50& Target:CaMK II ULK1 26.6 nM (IC 50 )
规格
规格或纯度
≥99%
英文名称
XST-14
生化机理
XST-14 是一种强效、竞争性和高选择性的 ULK1 抑制剂，其 IC 50 为 26.6 nM。XST-14 通过减少 ULK1 下游底物的磷酸化诱导自噬抑制。XST-14 可诱导肝细胞癌（HCC）细胞凋亡
储存条件
-20°C储存
运输条件
超低温运输
纯度
≥99%
名称和识别符
分子类型
小分子
Smiles
O=C(OC)C1=CC2=C(OC(C)C)C=C(OC(C)C)C=C2N1
分子量
291.34
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 250 mg/mL (858.10 mM; Need ultrasonic)
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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