Mitotan

SKU: orb1224775

Description

Mitotane(2,4′-DDD), an isomer of DDD and derivative of DDT, is an antineoplastic medication used in the treatment of adrenocortical carcinoma.(In Vitro):Mitotane (1 nM-100 μM; 6 days) significantly reduces H295R cell proliferation.Mitotane (10-100 μM; 6 or 48 h; TαT1 cells) reduces TαT1 cell viability in time- and dose-dependent manners; significantly and dose dependently increases caspase 3/7 activity from 60 μM to 80 μM; induced a significant and dose-dependent reduction in TSH secretion and TSH β-subunit mRNA expression from 40 μM to 100 μM.Mitotane (1-30 μM; 24 h; HepG2) increases transcription of the CYP3A4 and CYP2B6 gene in a dose-dependent manner.Mitotane (20 and 40 μM; 6 h) significantly reduces the number of neutral lipid droplets per cell in HepaRG, also induces a significant decrease in triacylglycerol-labeled lipid droplets; decreases the expression levels of PLIN1 and PLIN3.(In Vivo):Mitotane (440 mg/kg; i.p. or p.o,; 5 days a week, for 7 weeks) significantly reduces the volume of xenografts at an early time point after H295R cells inoculation.

Key Properties

• CAS Number: 53-19-0
• MW: 320.04
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₀Cl₄
• SMILES: ClC1=CC=C(C(C2=CC=CC=C2Cl)C(Cl)Cl)C=C1
• Target: AChR
• Solubility: Ethanol: 64 mg/mL warmed (199.97 mM); DMSO: 64 mg/mL (199.97 mM)

Bioactivity

• In Vivo:
  Animal model: NOD/SCID/γcnull mice (4-week-old; inoculated subcutaneously 6 × 106 H295R cells into the right flank). Dosage: 440 mg/kg. Administration: i.p. or p. o, ; 5 days a week, for 7 weeks. Result: Significantly reduced the volume of xenografts at an early time point (day 13) after H295R cells inoculation. The effect of oral mitotane treatment became non-significant by day 20 after H295R cells inoculation, while the effect of i.p. mitotane lasted until day 34.
• In Vitro:
  Cell Proliferation Assay Cell line: H295R cells. Concentration: 1 nM-100 μM. Incubation time: 6 days. Result: Significantly reduced H295R cell proliferation with an IC50 of 22.8 μM. Cell Viability Assay Cell line: TαT1 cells. Concentration: 10, 40, 60, 80 and 100 μM. Incubation time: 6 or 48 h. Result: Did not modify cell viability at 10-80 μM, while significantly (P < 0.01) reduced cell viability (-56%) at 100 μM, after 6 h incubation. Did not modify cell viability at 10-60 μM, whereas cell viability was significantly reduced at 60 μM (-31%; P < 0.05), 80 μM (-53%; P < 0.01), and 100 μM (-75.5%; P < 0.01), after 48 h incubation. RT-PCR Cell line: HepaRG cells and human hepatocytes. Concentration: 0.1, 1, 10, 20, 30, or 40 μM Incubation time: 24 or 48 h. Result: Increased mRNA levels of CYP3A4 and CYP2B6. Western blot analysis. Cell line: H295R. Concentration: 20, 40 and 50 μM. Incubation time: 6 h. Result: Decreased the expression levels of PLIN1 and PLIN3.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

o,p'-DDD | NSC 38721

Quick Database Links

Gene Symbol

AChR