1. Cell Cycle/DNA Damage Antibody-drug Conjugate/ADC Related
  2. DNA Alkylator/Crosslinker ADC Payload
  3. 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.

For research use only. We do not sell to patients.

seco-CBI-PBD dimer

seco-CBI-PBD dimer Chemical Structure

CAS No. : 550356-40-6

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Description

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.[1]

Cellular Effect
Cell Line Type Value Description References
CHO-AA8 IC50
0.054 nM
Compound: 27e
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
[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.

Cell Cytotoxicity Assay[1]

Cell Line: MES-SA, MES-SA/Dx5, BJAB, KPL-4, HCC1569 X2, T-47D, HCC1937, NCI-H1781, SW 900
Concentration: 0, 0.01, 0.1, 1, 10 and 100 nM
Incubation Time: 96 h
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).
Molecular Weight

576.08

Formula

C32H34ClN3O5

CAS No.
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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Purity & Documentation
References
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    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.

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Product Name:
seco-CBI-PBD dimer
Cat. No.:
HY-171718
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