Abemaciclib

SKU: orb1304526

Description

Abemaciclib methanesulfonate (LY2835219) is a potent and selective inhibitor of CDK4 (IC50=2 nM) and CDK6 (IC50=10 nM). It is widely used in cancer research, demonstrating activity in both in vitro cell proliferation assays and in vivo xenograft models for studying cell cycle progression and oncology therapeutics.

Research Area

Cell Biology

Key Properties

• CAS Number: 1231930-82-7
• MW: 602.70
• Purity: >98%
• Formula: C₂₇H₃₂F₂N₈·CH₃SO₃H
• SMILES: CS(O)(=O)=O.CCN1CCN(Cc2ccc(Nc3ncc(F)c(n3)-c3cc(F)c4nc(C)n(C(C)C)c4c3)nc2)CC1
• Target: Kinase
• Solubility: Soluble in DMSO (up to at least 25 mg/ml) or in Water (up to at least 25 mg/ml)

Bioactivity

• Target IC50:
  FLT3:3960 nM|CDK1-cyclinB1:1627 nM|HIPK2:31 nM|CDK5-p35:287 nM|CDK9-CyclinT1:57 nM|DYRK2:61 nM|CDK4:2 nM|DRAK1:659 nM|CDK5-p25:355 nM|PIM2:3400 nM|FLT3 (D835Y):403 nM|CDK2-CyclinE:504 nM|CK2:117 nM|CDK6:10 nM|GSK-3β:192 nM|CDK7-CyclinH-MAT1:3910 nM|PIM1:50 nM|JNK3:389 nM
• In Vivo:
  In retinoblastoma, LY2835219 inhibits cancer cell growth by specifically targeting and inhibiting CDK4 and CDK6, leading to cell cycle arrest at the G1 phase and suppression of DNA synthesis.
• In Vitro:
  In subcutaneous and intracranial glioma models (U87 mg), MsOH treatment results in LY2835219 inhibiting tumor growth in a dose-dependent manner.
• 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.

Storage & Handling

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

Alternative Names

LY2835219 mesylate

Compound Identifiers

PubChem CID

71576678