Abemaciclib

SKU: orb1305567

Description

Abemaciclib is a potent and selective CDK4/6 inhibitor (IC50=2/10 nM) with demonstrated antitumor activity. It is widely used in cancer research, particularly for studying advanced breast cancer, and has been validated in both in vitro cell proliferation assays and in vivo xenograft models.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1231929-97-7
• MW: 506.59
• Purity: 99.87% (May vary between batches)
• Formula: C₂₇H₃₂F₂N₈
• SMILES: C(C)(C)N1C=2C(=C(F)C=C(C2)C3=NC(NC4=CC=C(CN5CCN(CC)CC5)C=N4)=NC=C3F)N=C1C
• Target: CDK
• Solubility: DMSO:< 1 mg/mL (insoluble or slightly soluble);Ethanol:1.69 mg/mL (3.34 mM);10% DMSO+90% Saline:0.1 mg/mL (0.2 mM)

Bioactivity

• Target IC50:
  CDK2:504 nM|GSK3b:192 nM|DRAK1:659 nM|CDK4:2 nM|CDK5-p25:355 nM|DYRK2:61 nM|CDK9-CyclinT1:57 nM|FLT3:3960 nM|CDK7:3910 nM|CDK1-cyclinB1:1627 nM|CDK5-p35:287 nM|HIPK2:31 nM|CDK5:355 nM|CDK1:1627 nM|FLT3 (D835Y):403 nM|PIM2:3400 nM|JNK3:389 nM|PIM1:50 nM|CDK6:10 nM|CDK7-CyclinH-MAT1:3910 nM|GSK-3β:192 nM|CDK2-CyclinE:504 nM|CK2:117 nM
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• In Vivo:
  METHODS: To assay antitumor activity in vivo, Abemaciclib (45-90 mg/kg in 1% HEC in 20 mM phosphate buffer (pH 2.0)) was administered by gavage to BALB/c mice bearing human tongue squamous carcinoma tumors OSC-19 once daily for fourteen days. RESULTS: Abemaciclib significantly reduced tumor growth in OSC-19 xenografts during treatment. abemaciclib treatment decreased AKT phosphorylation but had no effect on mTOR activation. METHODS: To assay antitumor activity in vivo, Abemaciclib (22.5-90 mg/kg in 1% HEC in 25 mmol/L PB pH2) was administered by gavage to athymic nude mice harboring melanoma A375 once a day for twenty-one days. RESULTS: Statistically significant tumor growth inhibition was observed with Abemaciclib at 45 or 90 mg/kg dosing regimens. abemaciclib treatment significantly reduced pS780-Rb and pS10-Histone H3 levels, suggesting that CDK4/6 inhibition resulted in cell cycle inhibition and reduced tumor cell proliferation.
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• In Vitro:
  METHODS: HNSCC cell lines OSC-19, FaDu and YD-10B were treated with Abemaciclib (0.01-10 μM) for 72 h, and cell viability was measured by Cell Counting Kit. RESULTS: Abemaciclib treatment decreased the cell viability of HNSCC cells with IC50 values ranging from 0.5 μM to 0.7 μM. METHODS: AML cells MV4-11 were treated with Abemaciclib (0.04-5 μM) for 24 h. The cell cycle was detected using Flow Cytometry. RESULTS: Abemaciclib induced G1 phase block in MV4-11 cells. The G1-phase block was maximized when the concentration was ≥320 nmol/L. The RESULTS showed that Abemaciclib induced G1-phase block in MV4-11 cells.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cyclin dependent kinase, CDK, CDK6, CDK4, CDK4/6 dual inhibitor, Abemaciclib, inhibit, LY 2835219, LY2835219, LY-2835219, Inhibitor

Compound Identifiers

PubChem CID

46220502