seco-CBI-PBD dimer
seco-CBI-PBD dimer is a CBI-PBD heterodimer and a minor groove DNA crosslinker. seco-CBI-PBD dimer exhibits cytotoxicity against human tumor cells at sub-pM to low nM levels, shows low sensitivity to P-glycoprotein-mediated drug resistance, and can serve as an ADC payload. seco-CBI-PBD dimer can be used in studies of uterine cancer, breast cancer, non-small cell lung cancer, etc.
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- CAS No.: 550356-40-6
- Formule: C32H34ClN3O5
- Masse moléculaire:576.08
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Stockage:
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Activité biologique
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-AA8 | IC50 |
0.054 nM
Compound: 27e
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In vitro cellular toxicity against chinese hamster AA8 cell line after 4 hr of compound exposure
In vitro cellular toxicity against chinese hamster AA8 cell line after 4 hr of compound exposure
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[PMID: 12747786] |
In Vitro
Seco-CBI-PBD dimer (Compound 5) (0-100 nM; 96 h) potently inhibits proliferation of MES-SA, MES-SA/Dx5, BJAB, KPL-4, HCC1569 X2, T-47D, HCC1937, NCI-H1781, and SW 900 human tumour cell lines with IC50 values ranging from 0.0098 nM to 0.13 nM, completely suppresses proliferation at high concentrations, and has low sensitivity to P-glycoprotein-mediated resistance[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MES-SA, MES-SA/Dx5, BJAB, KPL-4, HCC1569 X2, T-47D, HCC1937, NCI-H1781, SW 900
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Concentration:0, 0.01, 0.1, 1, 10 and 100 nM
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Incubation Time:96 h
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Result:Exhibited potent cytotoxicity with IC50 values as follows: 0.033 nM (MES-SA), 0.11 nM (MES-SA/Dx5), 0.011 nM (BJAB), 0.036 nM (KPL-4), 0.13 nM (HCC1569 X2), 0.016 nM (T-47D), 0.11 nM (HCC1937), 0.0098 nM (NCI-H1781), 0.051 nM (SW 900).
Completely inhibited proliferation of all cell lines tested at sufficiently high concentrations.
Showed low sensitivity to P-glycoprotein overexpression, with an IC50 ratio of 3.3 between MES-SA/Dx5 (high P-glycoprotein) and MES-SA (P-glycoprotein-negative).
Chemical Information
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CAS No. 550356-40-6
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Masse moléculaire 576.08
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Formule C32H34ClN3O5
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SMILES
ClC[C@H]1C2=C(C=C(C3=CC=CC=C32)O)N(C1)C(CCCCCOC4=C(C=C5C(N=C[C@@]6([H])N(CCC6)C5=O)=C4)OC)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
seco-CBI-PBD dimer Related Classifications
HY-171718 Related Classifications
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