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Abemaciclib

CAS No. : 1231929-97-7

產(chǎn)品活性：Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC₅₀ values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

研究領(lǐng)域：Cell Cycle/DNA Damage

作用靶點(diǎn)：CDK

In Vitro: 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.

In Vivo: 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.

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