LY2835219 mesylate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LY2835219 是一种有效的选择性 CDK4 和 CDK6 抑制剂，在无细胞测定中 IC50 分别为 2 nM 和 10 nM。

LY2835219 is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3.(In Vitro):Abemaciclib (LY2835219) 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 (LY2835219) 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 (LY2835219) 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 (LY2835219) (45 mg/kg, p.o.) in combination with RAD001 causes a cooperative antitumor effect in HNSCC xenograft tumor. Abemaciclib (LY2835219) (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model.

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Abemaciclib

Angiogenesis

CDK

CDK4| CDK6

Cancer

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1231930-82-7

602.7

C27H32F2N8·CH4O3S

>98% (HPLC)

Ethanol: 24 mg/mL (39.82 mM); Water: 100 mg/mL (165.92 mM); DMSO: 83 mg/mL (137.71 mM)

CS(O)(=O)=O.CCN1CCN(CC2=CN=C(NC3=NC=C(F)C(=N3)C3=CC4=C(N=C(C)N4C(C)C)C(F)=C3)C=C2)CC1

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(-20℃)

With Ice Pack

≥ 2 years