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Abemaciclib  ≥99%

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包装规格：5mg 10mg 50mg 100mg in glass bottle
产品简介：Abemaciclib (LY2835219) 是具有选择性的 CDK4/6 抑制剂，能够抑制 CDK4/CDK6 的活性，IC50 分别为 2 nM 和 10 nM。
溶解性：DMSO :2.94 mg/mL (5.80 mM; ultrasonic and warming and heat to 80°C) Water： < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
储备液保存：-80°C, 6 months -20°C, 1 month (protect from light)
体内实验：1、请依序添加每种溶剂： 0.5% HEC Solubility: 3.33 mg/mL (6.57 mM); Suspended solution; Need ultrasonic ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
靶点：Cdk4/cyclin D1：2 nM (IC50) CDK6/cyclinD1： 10 nM (IC50) CDK9/cyclinT1：57 nM (IC50) CDK5/p35：287 nM (IC50) Cdk5/p25：355 nM (IC50) CDK2/cyclinE：504 nM (IC50) CDK7/Mat1/cyclinH1：3910 nM (IC50) CDK1/cyclinB1:1627 nM (IC50) PIM1:50 nM (IC50) PIM2:3400 nM (IC50) HIPK2:31 nM (IC50) DYRK2:61 nM (IC50) CK2:117 nM (IC50) GSK3b:192 nM (IC50) JNK3:389 nM (IC50) FLT3 (D835Y):403 nM (IC50) FLT3:3960 nM (IC50) DRAK1:659 nM (IC50)
体外研究：Abemaciclib reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells. Abemaciclib shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM; Abemaciclib inhibits the proliferation of the parental A375 and resistant A375RV1 and A375RV2 cells with similar potencies with IC50 values of 395, 260, and 463 nM, respectively. Abemaciclib inhibits CDK4 and CDK6 with low nanomolar potency, inhibits Rb phosphorylation resulting in a G1 arrest and inhibition of proliferation, and its activity is specific for Rb-proficient cells.
体内研究：Abemaciclib (45 mg/kg, p.o.) in combination with RAD001 causes a cooperative antitumor effect in HNSCC xenograft tumor. Abemaciclib (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model.
保存条件：2-8°C 避光
注意事项：1、为了您的安全和健康，请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。

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