Estramustine phosphate sodium

SKU: orb1222120

Description

Estramustine phosphate sodium is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2/M phase of the cell cycle.(In Vitro):Estramustine phosphate sodium (1 μg/ mL, 48 h) suppresses PC3 cell growth.Estramustine phosphate sodium (2 μg/mL, 48 h) elevates phosphatidylserine eversion amount on PC3 cells and induces PC3 cell apoptosis through reducing miR-31.Estramustine phosphate sodium (0-40 μM, 24-72 h) inhibits cell proliferation and tubulin cytoskeleton in RAW 264.7 cells.Estramustine phosphate sodium (10 μM, 24 h) inhibits TGF-β-induced RAW 264.7 cell migration, as well as TGF-β-induced uPA production by inhibiting Smad3 activation.(In Vivo):Estramustine phosphate sodium (Intraperitoneal injection, 4 or 12 mg/kg, a daily dose for 2 weeks) inhibits PAC120 tumor growth 53% by day 35.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 52205-73-9
• MW: 564.35
• Purity: >98% (HPLC)
• Formula: C₂₃H₃₀Cl₂NNa₂O₆P
• SMILES: [Na+].[Na+].ClCCN(CCCl)C(=O)Oc3cc4CC[C@@H]1[C@H](CC[C@]2(C)[C@H](CC[C@@H]12)OP([O-])([O-])=O)c4cc3
• Target: Caspase
• Solubility: H2O : 62.5 mg/mL 110.75 mM;DMSO : 5 mg/mL 8.86 mM

Bioactivity

• In Vivo:
  Estramustine phosphate sodium (Intraperitoneal injection, 4 or 12 mg/kg, a daily dose for 2 weeks) inhibits PAC120 tumor growth 53% by day 35. Animal model: Swiss nu/nu (nude) male mice (5-week-old) bearing PAC120 tumors. Dosage: 4 mg/kg, 12 mg/kg. Administration: Intraperitoneal injection; daily; for 2 weeks. Result: Suppressed the development of skin lesions and resulted in a dissociation between DTH response and antibody production. Animal model: Human prostate cancer xenograft PAC120. Dosage: 4 or 12 mg/kg, a daily dose for 2 weeks. Administration: Intraperitoneal injection. Result: Inhibited PAC120 tumor growth 53% by day 35.
• In Vitro:
  Estramustine phosphate sodium (1 μg/ mL, 48 h) suppresses PC3 cell growth. Estramustine phosphate sodium (2 μg/mL, 48 h) elevates phosphatidylserine eversion amount on PC3 cells and induces PC3 cell apoptosis through reducing miR-31.Estramustine phosphate sodium (0-40 μM, 24-72 h) inhibits cell proliferation and tubulin cytoskeleton in RAW 264.7 cells. Estramustine phosphate sodium (10 μM, 24 h) inhibits TGF-β-induced RAW 264.7 cell migration, as well as TGF-β-induced uPA production by inhibiting Smad3 activation. Cell Viability Assay Cell line: PC3 cells. Concentration: 1 μg/ mL. Incubation time: 48 h. Result: Suppressed PC3 cell growth. Immunofluorescence Cell line: RAW 264.7 cells Concentration: 10 μM. Incubation time: 24 h. Result: Disrupted the interphase microtubules. Cell Migration Assay Cell line: 18 h of TGF-β treated RAW 264.7 cells Concentration: 10 μM. Incubation time: 24 h. Result: Inhibited TGF-β-Induced Cell Migration.

Storage & Handling

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

Quick Database Links

Gene Symbol

Caspase