Lobaplatin (D-19466)

SKU: orb1220236

Description

Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexes. Lobaplatin (D-19466) shows activity for a variety of tumour types and is a promising antitumour chemotherapeutic agent.

Key Properties

• CAS Number: 135558-11-1
• MW: 397.33
• Purity: >98% (HPLC)
• Formula: C?H??N?O?Pt
• SMILES: CC1[O-][Pt+2]2([NH2]CC3C(CC3)C[NH2]2)[O-]C1=O
• Solubility: H2O : ≥ 50 mg/mL (125.84 mM; DMSO can inactivate Lobaplatin's activity)

Bioactivity

• In Vivo:
  Lobaplatin (5 and 10 mg/kg; i.p.; once a week, for 3 weeks) suppresses tumor growth of esophageal squamous cell carcinoma (ESCC) xenograft. Animal model: Male BALB/c nude mice (4-6 weeks) with ESCC xenograft. Dosage: Intraperitoneal injection; once a week, for 3 weeks. Administration: 5 and 10 mg/kg. Result: Suppressed tumor volumes in a dose-dependent manner. Increased expressions of Bax and decreased expressions of Bcl-2.
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• In Vitro:
  Lobaplatin (D-19466, 0.25-32 μg/mL; 24-72 h) exhibits anti-proliferative activities against esophageal squamous cell carcinoma (ESCC) cell lines. Lobaplatin (0-16 μg/mL; 48 h) induces esophageal squamous cell carcinoma (ESCC) apoptosis and modulates expression of apoptosis-related proteins. Lobaplatin (1.45 μg/mL; 0-48 h; SMMC-7721 cells) arrests cell cycle progression at G1 and G2/M phases in a time-dependent manner. Lobaplatin (1.45 μg/mL; 0-48 h; SMMC-7721 cells) inhibits the mRNA levels of cyclin B, CDK1, and CDC25C phosphatase, down-regulates Rb/E2F complexes and up-regulates of CDK inhibitors. TCell Viability Assay Cell line: KYSE-410 cells and EC-109 cells. Concentration: 0.25, 0.5, 1, 2, 4, 8, 16 and 32 μg/mL Incubation time: 24, 48 and 72 hours. Result: Inhibited the growth of KYSE-410 and EC-109 cells in a dose- and time-dependent manner. Inhibited the clone formation activity of KYSE-410 and EC-109 cells in a dosedependent manner. Apoptosis Analysis Cell line: KYSE-410 cells and EC-109 cells. Concentration: 0.25, 1, 4 and 16 μg/mL Incubation time: 48 hours. Result: Increased the percentage of apoptotic cells in a dose-dependent manner. Western blot analysis. Cell line: KYSE-410 cells and EC-109 cells. Concentration: 0, 1, 4 and 16 μg/mL. Incubation time: 48 hours. Result: Increased expressions of cleaved-caspase-3, cleaved-caspase-8, cleaved-caspase-9 and Bax, while decreased expression of Bcl-2.Cell Cycle Analysis Cell line: SMMC-7721 cells. Concentration: 1.45 μg/mL Incubation time: 0, 24, 36 and 48 hours. Result: Arrested the proportions of G1, S, and G2/M phases in cells were 45.31, 22.88, and 31.81% at 0 h, 59.91, 11.92, and 28.17% at 24 h, 56.89, 2.83, and 40.28% at 36 h, and 53.80, 2.07, and 44.13% at 48 h, respectively. Western blot analysis. Cell line: SMMC-7721 cells. Concentration: 1.45 μg/mL Incubation time: 0, 24, 36 and 48 hours. Result: Down-regulated cyclin B, CDK1, CDC25C, phosphorylated CDK1 (pCDK1), pCDK4, Rb, E2F, and pRb, and up-regulated p53, p21, and p27.
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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

D-19466