Cerivastatin

SKU: orb1707467

Description

Cerivastatin is a potent, orally active HMG-CoA reductase inhibitor used to study hyperlipidemia and cancer. It effectively lowers LDL cholesterol and has demonstrated in vitro activity against the proliferation and invasion of breast cancer cell lines like MDA-MB-231.

Research Area

Cell Biology, Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 145599-86-6
• MW: 459.55
• Purity: 99.56% (May vary between batches)
• Formula: C₂₆H₃₄FNO₅
• SMILES: C(=C/[C@H](C[C@H](CC(O)=O)O)O)\C=1C(=C(COC)C(C(C)C)=NC1C(C)C)C2=CC=C(F)C=C2
• Target: Ferroptosis,HMG-CoA Reductase

Bioactivity

• Target IC50:
  HMG-CoA reductase:1.3 nM/L (Ki)
• In Vivo:
  Trametinib and Cerivastatin were initially dissolved in DMSO and diluted into an aqueous pooled dose containing a final concentration of 0.5% hypromellose and 0.05% Tween-80, in saline. Generated xenografts of a primary monosomic BAP1-mutated human UM cell line, UPMM3, in highly immunodeficient NOD.Cg-Prkdcscid Il2rgtm1wjl/SzJ mice to validate the effects of trametinib and Cerivastatin combination on UM cells in vivo. One week after subcutaneous injection of UPMM3 cells, when the tumour was palpable, four mice per group were treated with vehicle, trametinib (1 mg/kg, per os, three days/week), Cerivastatin (2 mg/kg per os, three days/week) or trametinib and Cerivastatin for 57 days (until day 64). The end of treatment was followed by 15 days of observation. The addition of Cerivastatin determined a significantly stronger inhibition of tumour growth compared with mice treated with trametinib alone (p = 0.03).
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• In Vitro:
  Cerivastatin induced a dose-dependent decrease in cell proliferation of MDA-MB-231 cells (up to 40% inhibition at 25 ng/ml). In contrast, Cerivastatin treatment did not significantly modify MCF-7 cell proliferation. Flow cytometry analysis showed that Cerivastatin induced an arrest of the cell cycle in G 1 /S phase (67.1% in Cerivastatin -treated cells) after 36 h treatment.
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Storage & Handling

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

Alternative Names

Ferroptosis, HMGCoAReductase, HMG-CoA Reductase (HMGCR), HMGCoA Reductase, Cerivastatin

Compound Identifiers

PubChem CID

446156