Lobaplatin (D-19466)

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

洛铂 (D-19466) 是铂 (II) 络合物的非对映混合物。 Lobaplatin (D-19466) 对多种肿瘤类型具有活性，是一种有前途的抗肿瘤化疗化合物。

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.

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/mLIncubation 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.

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.

D-19466

Others

Other Targets

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135558-11-1

397.33

C?H??N?O?Pt

>98% (HPLC)

H2O : ≥ 50 mg/mL (125.84 mM; DMSO can inactivate Lobaplatin's activity)

CC1[O-][Pt+2]2([NH2]CC3C(CC3)C[NH2]2)[O-]C1=O

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(-20℃)

With Ice Pack

≥ 2 years