JNJ-27548547
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.
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- CAS. Nr.: 303983-00-8
- Formel: C62H98N4O11S2
- Molecular Weight:1139.59
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Pegylated liposomal JNJ-27548547 (Compound PL-MLP) (72 h) has substantially reduced in vitro cytotoxicity against mouse M109 carcinoma cells under standard conditions, but its cytotoxicity increases up to 6-fold to near-free MMC levels when co-incubated with 0.25-1.0 mM Cysteine (HY-Y0337) or N-acetyl-cysteine (HY-B0215) (72 h)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:mouse M109 carcinoma cells
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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
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Incubation Time:72 h (PL-MLP continuous exposure); 72 h (co-incubation with reducing agents)
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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.
Pegylated liposomal JNJ-27548547 (4-8 mg/kg; i.v.; single dose, day 5 after tumor inoculation) demonstrates significant antitumor activity in the C26 colon carcinoma model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:2, 5 mg/kg (single dose); 2, 4 mg/kg (3 doses); 6 mg/kg (2-3 doses)
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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)
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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).
Chemical Information
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CAS. Nr. 303983-00-8
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Molecular Weight 1139.59
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Formel C62H98N4O11S2
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SMILES
CO[C@]12[C@]3([H])[C@@](CN1C4=C(C(C(N)=C(C4=O)C)=O)[C@H]2COC(N)=O)([H])N3C(OCC5=CC=C(SSCC(OC(CCCCCCCCCCCCCCCCC)=O)COC(CCCCCCCCCCCCCCCCC)=O)C=C5)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
JNJ-27548547 Related Classifications
HY-185585 Related Classifications
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