Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan
Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan (Compound 11) is a bioactive compound-linker conjugate for ADC. Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan can conjugate with antibodies to form ADC (C-11) with anti-tumor activity. Exatecan is a DNA Topoisomerase I inhibitor. Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan can be used in the research of squamous cell carcinoma, pancreatic adenocarcinoma and colorectal cancer.
For research use only. We do not sell to patients.
- CAS No.: 2578019-72-2
- Formula: C55H60FN9O13
- Molecular Weight:1074.12
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
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Camptothecins |
In Vitro
Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan (1 nM - 1 μM; 72 h) inhibits proliferation of Fadu, Bxpc-3, A431, and SW620 human tumor cell lines in vitro with IC50 values ranging from 12.44 nM to 242.09 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Fadu, Bxpc-3, A431, SW620 human tumor cell lines
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Concentration:1 nM - 1 μM (5-fold serial dilutions, 9 concentrations total)
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Incubation Time:72 h
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Result:Inhibited proliferation of Fadu cells with an IC50 of 12.44 nM.
Inhibited proliferation of Bxpc-3 cells with an IC50 of 242.09 nM.
Inhibited proliferation of A431 cells with an IC50 of 27.86 nM.
Inhibited proliferation of SW620 cells with an IC50 of 221.24 nM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (4~6 weeks old)[1]
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Dosage:10 mg/kg
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Administration:i.v.; on days 0, 7, 14, 21
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Result:Reduced average tumor volume to 347.2 mm3 on day 20, compared to 1526.5 mm3 in the blank control group.
Increased average body weight from 17.6 g on day 0 to 20.1 g on day 20.
Showed no significant weight loss or mouse mortality during the study.
Chemical Information
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CAS No. 2578019-72-2
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Molecular Weight 1074.12
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Formula C55H60FN9O13
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SMILES
O=C(C1CCC(CC1)CN2C(C=CC2=O)=O)NCC(NCC(N[C@@H](CC3=CC=CC=C3)C(NCC(NCO[C@@H](C)C(N[C@@H]4C5=C6C(C(N7C6)=CC([C@](O)(C(OC8)=O)CC)=C8C7=O)=NC9=CC(F)=C(C)C(CC4)=C95)=O)=O)=O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)