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抑制剂/激活剂

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凋亡与自噬

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Abemaciclib LY2835219

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。

货号：
TK0105
规格：

1mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	1231929-97-7
生物活性	Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
分子式	C27H32F2N8
分子量	506.59
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	4°C, protect from light
溶解性数据	DMSO : 5 mg/mL (9.87 mM; Need ultrasonic)
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.
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.
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纯度及产品资料	98%

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