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 是一种 CBI-PBD 异源二聚体和 DNA 小沟交联剂。seco-CBI-PBD dimer 对人类肿瘤细胞具有亚 pM 至低 nM 的细胞毒性,且对 P-糖蛋白介导的耐药性敏感性较低,可用于 ADC 有效载荷。seco-CBI-PBD dimer 可用于子宫癌、乳腺癌、非小细胞肺癌等研究。

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seco-CBI-PBD dimer

seco-CBI-PBD dimer Chemical Structure

CAS No. : 550356-40-6

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  • 生物活性

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生物活性

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]

体外研究
(In Vitro)

Seco-CBI-PBD dimer (Compound 5) (0-100 nM; 96 h) 可强效抑制 MES-SA、MES-SA/Dx5、BJAB、KPL-4、HCC1569 X2、T-47D、HCC1937、NCI-H1781 和 SW 900 人肿瘤细胞系的增殖,其 IC50 值范围为 0.0098 nM 至 0.13 nM;在高浓度下可完全抑制细胞增殖,且对 P-糖蛋白介导的耐药性敏感性较低[1]

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).
分子量

576.08

Formula

C32H34ClN3O5

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
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  • 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.

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产品名称:
seco-CBI-PBD dimer
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HY-171718
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