Lerociclib

SKU: orb1709651

Description

Lerociclib

Research Area

Cell Biology

Key Properties

• CAS Number: 1628256-23-4
• MW: 474.6
• Purity: 99.56% (May vary between batches)
• Formula: C₂₆H₃₄N₈O
• SMILES: O=C1NCC2(N3C=4N=C(N=CC4C=C13)NC5=NC=C(C=C5)N6CCN(CC6)C(C)C)CCCCC2
• Target: CDK

Bioactivity

• Target IC50:
  Cdk4-CyclinD1:1 nM|CDK5-p35:0.832 μM|CDK6-CyclinD3:2 nM|CDK1-cyclinB1:2.4 μM|CDK5-p25:1.2 μM|CDK2-CyclinE:3.6 μM|CDK7-CyclinH-MAT1:2.4 μM|CDK4/6 dependent cells:20 nmol/L (EC50)|CDK9-CyclinT:28 nM|CDK2-CyclinA:1.5 μM
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• In Vivo:
  To evaluate the murine PK/PD relationship of Lerociclib, an ER+ MCF7 xenograft model was utilized. Compound concentrations were measured in plasma and tumors from tumor-bearing mice given a single oral dose of Lerociclib (100 mg/kg). Oral Lerociclib has sufficient mouse PK/PD for assessing efficacy in tumor models.
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• In Vitro:
  Lerociclib is highly potent and selective for CDK4/cyclin D1 and CDK6/cyclin D3 over CDK1, CDK2, CDK5 and CDK7 and their respective binding partners. Lerociclib produced a robust and sustained G1 arrest in CDK4/6 dependent cells with an EC50 of ~20 nmol/L.
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Storage & Handling

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

Alternative Names

CDK9/Cyclin T, CDK4, Cdk4/cyclin D1, cdk6/cyclin D3, CDK7/Cyclin H/MAT1, CDK6, CDK5/p35, Cdk5/p25, cdk2/cyclin A, CDK2/cyclinE, CDK1/cyclinB1, G1T 38, G1T38, G1T-38, Lerociclib

Compound Identifiers

PubChem CID

86269224