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Casein Kinase inhibitor A86
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Casein Kinase inhibitor A86图片
CAS NO:2079069-01-3
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
Casein Kinase inhibitor A86 是一种有效且具有口服活性的酪蛋白激酶 1α (CK1α) 抑制剂。Casein Kinase inhibitor A86 还抑制 CDK7 (TFIIH) 和 CDK9 (P-TEFb)。Casein Kinase inhibitor A86 可诱导白血病细胞凋亡 (apoptosis)，并具有有效的抗白血病活性。
Cas No.2079069-01-3
分子式C18H25FN6
分子量344.43
溶解度DMSO : 12.5 mg/mL (36.29 mM; ultrasonic and warming and heat to 60°C)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities[1].

Casein Kinase inhibitor A86 is highly effective in inducing leukemia cell apoptosis at 160 nM or lower, mostly in correlation to their capacity to stabilize p53[1].Casein Kinase inhibitor A86 (0.08-2 μM; 6.5 hours) abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1. Casein Kinase inhibitor A86 induces a marked reduction in mRNA expression of MYC and MDM2, yet upregulates the expression of the Wnt targets AXIN2 and CCND1 (Cyclin D1)[1].

Pharmacokinetic studies of the inhibitor Casein Kinase inhibitor A86 at 20 mg/kg reveal rapid oral absorption with a Tmax of 0.2-0.5 hr, Cmax of 1115 ng/mL, T1/2 of 4.3 hr, and area under the curve (AUC) values of 2606 (ng*hr/mL)[1].

[1]. Waleed Minzel, et al. Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. Cell. 2018 Sep 20;175(1):171-185.e25.