Casein Kinase inhibitor A86|2079069-01-3|-陌孚医药/Medlife

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Casein Kinase inhibitor A86

目录号: PL13961 纯度: ≥98%

CAS No. :2079069-01-3

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中文名称	Casein Kinase inhibitor A86
英文名称	Casein Kinase inhibitor A86
英文别名	Casein Kinase inhibitor A86;LCI;[4-[[4-[5-(cyclopropylmethyl)-1-methyl-pyrazol-4-yl]-5-fluoranyl-pyrimidin-2-yl]amino]cyclohexyl]azanium;(1R,4r)-N1-(4-(5-(cyclopropylmethyl)-1-methyl-1H-pyrazol-4-yl)-5-fluoropyrimidin-2-yl)cyclohexane-1,4-diamine
Cas No.	2079069-01-3
分子式	C₁₈H₂₅FN₆
分子量	344.43
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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。
生物活性	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.
性状	Solid
IC50 & Target[1][2]	CKIα CDK7 0.31 nM (Kd)
体外研究(In Vitro)	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. 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). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Pharmacokinetic studies of the inhibitor Casein Kinase inhibitor A86 at 20 mg/kg reveal rapid oral absorption with a T max of 0.2-0.5 hr, C max of 1115 ng/mL, T 1/2 of 4.3 hr, and area under the curve (AUC) values of 2606 (ng*hr/mL). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[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.

溶解度数据	In Vitro: DMSO : 12.5 mg/mL (36.29 mM; ultrasonic and warming and heat to 60°C)配制储备液

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