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  4. JNJ-27548547

JNJ-27548547，Mitomycin C (HY-13316) 前药，是一种 Mitomycin C 和亲酯基团的偶联物。JNJ-27548547 在还原剂存在下其二硫苄基连接键会发生硫解断裂，从而释放出活性物质 Mitomycin C。JNJ-27548547 被制备为聚乙二醇化脂质体 (PL-MLP)，在小鼠模型中具有高抗肿瘤活性。

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JNJ-27548547

JNJ-27548547 Chemical Structure

CAS No. : 303983-00-8

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JNJ-27548547 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JNJ-27548547, Mitomycin C (HY-13316) prodrug, is a Mitomycin C and lipophilic group conjugate. JNJ-27548547 undergoes thiolytic cleavage of its dithiobenzyl linker in the presence of reducing agents to release active substance Mitomycin C. JNJ-27548547 is formulated into pegylated liposomes (PL-MLP) with high antitumor activity in mice models[1].

体外研究
(In Vitro)

聚乙二醇化脂质体 JNJ-27548547 (Compound PL-MLP) (72 h) 在标准条件下对小鼠 M109 癌细胞的体外细胞毒性显著降低，但当与 0.25-1.0 mM Cysteine (HY-Y0337) 或 N-acetyl-cysteine (HY-B0215) (72 h) 时，其细胞毒性可升高至近游离 MMC 水平的 6 倍[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

JNJ-27548547 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: mouse M109 carcinoma cells
Concentration: MMC equivalents (PL-MLP); 0.25-1.0 mM cysteine; 0.25-1.0 mM N-acetyl-cysteine; 0.25-1.0 mM mesna
Incubation Time: 72 h (PL-MLP continuous exposure); 72 h (co-incubation with reducing agents)
Result: Exhibited 5- to 6-fold less cytotoxicity than free mitomycin C (MMC) under standard conditions.
Increased cytotoxic activity by up to 6-fold, reaching levels nearly comparable to free MMC, when co-incubated with 0.25 to 1.0 mM cysteine or N-acetyl-cysteine.
体内研究
(In Vivo)

聚乙二醇化脂质体 JNJ-27548547 (Compound PL-MLP) (静脉注射；单剂量、2 次给药、3 次给药，剂量 2-6 mg/kg) 在 M109 肺癌足垫模型中表现出剂量依赖性抗肿瘤活性；当于第 5、12 和 19 天以 6 mg/kg 剂量静脉注射给药时，治愈率达 30%，且无相关毒性死亡发生[1]。
聚乙二醇化脂质体 JNJ-27548547 (4-8 mg/kg；静脉注射；单次给药，肿瘤接种后第 5 天) 在 C26 结肠癌腹腔模型中表现出显著的抗肿瘤活性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Lung carcinoma BALB/c mice (female, 8 weeks old, M109 lung carcinoma cells inoculated into hind footpad at 10^6 cells per mouse)[1]
Dosage: 2, 5 mg/kg (single dose); 2, 4 mg/kg (3 doses); 6 mg/kg (2-3 doses)
Administration: i.v.; single dose (day 7); 3 doses (days 7, 14, 21); 2 doses (days 5, 12); 2-3 doses (days 5, 12, 19)
Result: Extended median time to tumor >5 mm or death to 27 days; yielded 0% cures and 0% toxic deaths (n=20).
Extended median time to tumor >5 mm or death to 32 days; yielded 0% cures and 0% toxic deaths (n=21).
Extended median time to tumor >5 mm or death to 34 days; yielded 0% cures and 0% toxic deaths (n=10).
Extended median time to tumor >5 mm or death to 44 days; yielded 0% cures and 0% toxic deaths (n=10).
Extended median time to tumor >5 mm or death to 61 days; yielded 0% cures and 0% toxic deaths (n=10).
Extended median time to tumor >5 mm or death to 62 days; yielded 30% cures and 0% toxic deaths (n=20).
分子量

1139.59

Formula

C62H98N4O11S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

JNJ-27548547 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JNJ-27548547303983-00-8JNJ27548547JNJ 27548547Drug IntermediateDrug IintermediateBALB/c miceSprague-Dawley ratsC26colon carcinomareducing agentsM109 carcinomamitomycin CM109Rpegylated liposomescarcinomaInhibitorinhibitorinhibit

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