Ribociclib hydrochloride

SKU: orb1707087

Description

Ribociclib hydrochloride (LEE011 HCl) is an orally bioavailable, potent CDK4/6 inhibitor with IC50 values of 10 and 39 nM, respectively. It arrests the cell cycle in G1 phase and is widely used in cancer research, including in vitro proliferation assays and in vivo xenograft studies for breast cancer and other malignancies.

Research Area

Cell Biology

Key Properties

• CAS Number: 1211443-80-9
• MW: 471
• Purity: 99.87%
• Formula: C₂₃H₃₁ClN₈O
• SMILES: Cl.O=C(C1=CC=2C=NC(=NC2N1C3CCCC3)NC4=NC=C(C=C4)N5CCNCC5)N(C)C
• Target: CDK,Cell Cycle Arrest
• Solubility: H2O:8 mg/mL (16.99 mM);DMSO:5.8 mg/mL (12.31 mM)

Bioactivity

• Target IC50:
  CDK4:10 nM|CDK6:39 nM
• In Vivo:
  In CB17 immunodeficient mice bearing BE2C, NB-1643, or EBC1 parazacco spilurus subsp. spilurus xenografts, the dosing regimen of Ribociclib hydrochloride (200 mg/kg, oral gavage, for 21 days) was well tolerated, with no body weight loss or other toxic reactions observed in any xenograft model mice. During the 21-day treatment period, tumor growth was significantly inhibited in mice bearing BE2C or NB-1643 xenografts, though tumor regrowth occurred after drug withdrawal. In contrast, the tumor growth inhibitory effect was not significant in the EBC1 xenograft model .
• In Vitro:
  Ribociclib hydrochloride (LEE011) significantly inhibited the anchorage-dependent growth of 12 out of 17 neuroblastoma cell lines. Following treatment with Ribociclib hydrochloride (100 nM and 250 nM), neuroblastoma cell lines known to be sensitive to CDK4/6 inhibition (BE2C and IMR5) exhibited significant accumulation of cells in the G0/G1 phase of the cell cycle .

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK4, CDK6, LEE011 hydrochloride, LEE-011 Hydrochloride, LEE 011 hydrochloride, Ribociclib Hydrochloride

Compound Identifiers

PubChem CID

67242274