计算溶液所需的质量、体积或浓度。
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
Casein Kinase inhibitor A51 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A51 induces leukemia cell apoptosis , and has potent anti-leukemic activities
In Vitro
Similar to CKIα depletion, Casein Kinase inhibitor A51 (0.05-3.2 μM; 18 hours) treatment of RKO cells abolished most of the Ser45 phosphorylation signal and the consecutive GSK3 phosphorylation cascade resulting in stabilization of β-catenin. Casein Kinase inhibitor A51 is highly effective in inducing leukemia cell apoptosis at 160 nM or lower, mostly in correlation to their capacity to stabilize p53. Casein Kinase inhibitor A51 (0.08-2 μM; 6.5 hours) abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1. Casein Kinase inhibitor A51 induces a marked reduction in mRNA expression of MYC and MDM2, yet upregulates the expression of the Wnt targets AXIN2 and CCND1 (Cyclin D1). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MV4-11 cells Concentration: 0.08 μM, 0.6 μM, 2 μM Incubation Time: 6.5 hours Result: Abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1.
In Vivo
Oral treatment is initiated at 8 days (Casein Kinase inhibitor A51; 5 mg/kg/day) after leukemia cell inoculation, at which the percentage of leukemia cells in the BM is more than 1.5% of all cells. all A51-treated mice have normal organ morphology and histology and normal blood counts . Pharmacokinetic studies of the inhibitor Casein Kinase inhibitor A51 at 20 mg/kg reveal rapid oral absorption with a T max of 0.5-2 hr, C max of 1060 ng/mL, T 1/2 of 2.5 hr, and area under the curve (AUC) values of 3680 (ng*hr/mL) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:CKIα CDK7 1.3 nM (Kd) CDK9 4 nM (Kd)
规格
别名
酪蛋白激酶抑制剂 A51
规格或纯度
10mM in DMSO
英文名称
Casein Kinase inhibitor A51
生化机理
酪蛋白激酶抑制剂 A51 是一种强效的口服活性酪蛋白激酶 1α （CK1α）抑制剂。酪蛋白激酶抑制剂 A51 能诱导白血病细胞凋亡，具有强效抗白血病活性。
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
CN1C(=C(C=N1)C2=NC(=NC=C2Cl)NC3CCC(CC3)N)CC4CC4
PubChem CID
分子量
360.88
技术文档
高级数据
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
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 保留所有权利。
危险品化学品经营许可证（带存储）