Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively.
IC50&Target
Cdk4/cyclin D1
2 nM (IC50)
CDK6/cyclinD1
10 nM (IC50)
CDK2/cyclinE
504 nM (IC50)
CDK9/cyclinT1
57 nM (IC50)
CDK1/cyclinB1
1627 nM (IC50)
CDK7/Mat1/cyclinH1
3910 nM (IC50)
Cdk5/p25
355 nM (IC50)
CDK5/p35
287 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 (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.
体内研究
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.
分子式
C27H32N8F2.CH4O3S
分子量
602.70
CAS号
1231930-82-7
运输条件
Room temperature in continental US; may vary elsewhere.