Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Abemaciclib (CDK4/6 dual inhibitor) is an effective and specific CDK4/6 inhibitor (IC50: 2/10 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 48.00 | |
25 mg | In stock | $ 78.00 | |
50 mg | In stock | $ 97.00 | |
100 mg | In stock | $ 126.00 | |
200 mg | In stock | $ 158.00 | |
500 mg | In stock | $ 288.00 | |
1 g | In stock | $ 427.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 77.00 |
Description | Abemaciclib (CDK4/6 dual inhibitor) is an effective and specific CDK4/6 inhibitor (IC50: 2/10 nM). |
Targets&IC50 | CDK4:2 nM, CDK6:10 nM |
In vitro | 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[1]. LY2835219 shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM; LY2835219 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[2]. 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[3]. |
In vivo | LY2835219 (45 mg/kg, p.o.) in combination with everolimus causes a cooperative antitumor effect in HNSCC xenograft tumor[1]. LY2835219 (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model[2]. |
Kinase Assay | Cells (5×103) are plated in 96 well plates. Cells are treated the next day for 24 to 48 hours and then assessed for caspase-3 activity by Caspase-Glo-3/7 Assay, as per manufacturer's instructions and a luminescence plate reader. |
Cell Research | LY2835219 is dissolved in DMSO to a 10 mM concentration.? Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer's instructions. The interaction between LY2835219 and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of <1 is synergistic and a CI of >1 is antagonistic. |
Synonyms | CDK4/6 dual inhibitor, LY2835219 |
Molecular Weight | 506.59 |
Formula | C27H32F2N8 |
CAS No. | 1231929-97-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10mg/mL(19.74mM)
Ethanol: 5.06mg/mL (10mM)
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Abemaciclib 1231929-97-7 Cell Cycle/Checkpoint CDK inhibit CDK4/6 dual inhibitor LY 2835219 LY2835219 Inhibitor LY-2835219 Cyclin dependent kinase inhibitor