| DC39818 |
CL2-SN-38(DCA)
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CL2-SN-38 is a cleavable linker-based antibody-drug conjugate (ADC) containing the topoisomerase I inhibitor SN-38 and a maleimidocaproyl linker. CL2-SN-38 has been linked to tumor-selective human monoclonal antibodies, such as anti-CEACAM5 (hMN-14) to target SN-38 to tumor sites and improve its solubility. CL2-SN-38 linked to hMN-14 binds (Kd = 1.4 nM) and is cytotoxic to LoVo human colon adenocarcinoma cells (IC50 = 5.3 nM). CL2-SN-38 linked to hMN-14 increases survival in a colon carcinoma mouse model of lung metastasis. |
| DC50025 |
Deruxtecan
|
Deruxtecan, a topoisomerase I inhibitor, is an exatecan derivative (DX-8951 derivative) with a cleavable pepetide linker and a maleimide group. The maleimide group in Deruxtecan can react with antibody to form antibody-drug conguates (ADC) such as Trastuzumab deruxtecan (DS-8201a), which is a HER2-targeting antibody–drug conjugate. |
| DC45695 |
Thailanstatin A
|
Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50=650 nM). Thailanstatin A exerts effects via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome and shows low-nM to sub-nM IC50s against multiple cancer cell lines. Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding “linker-less” ADC. |
| DC44783 |
7-Aminomethyl-10-methyl-11-fluoro camptothecin
|
7-Aminomethyl-10-methyl-11-fluoro camptothecin is a cytotoxin of MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin. 7-Aminomethyl-10-methyl-11-fluoro camptothecin can be used for the synthesis of camptothecin antibody-drug conjugate (ADC).
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| DC40467 |
Mytoxin B
|
Mytoxin B is an ADC cytotoxin. Mytoxin B is a satratoxin-type trichothecene macrolide and is similar to the effect of LY294002. Mytoxin B induces cell apoptosis via PI3K/Akt pathway.
|
| DC7648 |
PNU159682
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PNU-159682 is a major bioactive metabolite of Nemorubicin in human liver microsomes; > 3,000-fold cytotoxic than its parent compound(MMDX and doxorubicin). |
| DC8241 |
Ansamitocin P-3
|
Ansamitocin P-3, a potent anti-tumor maytansinoid found in Actinosynnema pretiosum, is a maytansine analog which displays potent cytotoxicity against the human solid tumor cell lines A-549 and HT-29. |
| DC8540 |
DM-1(Mertansine)
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A cytotoxic agent used in antibody-drug conjugates |
| DC72886 |
Dox-btn2
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Dox-btn2 is a biotinylated derivative of Doxorubicin, with a biotin label at the point of conjugation to doxorubicin at 3'-NH2. Dox-btn2 can be used for cell imaging. While Doxorubicin is mainly accumulated in the nucleus, while Dox-btn2 is mainly located in the cytoplasm. |
| DC72753 |
Gly-Cyclopropane-Exatecan
|
Gly-Cyclopropane-Exatecan involves in the synthesis of anti-B7-H4 ADC, containing Exatecan, a DNA Topoisomerase I inhibitor. Gly-Cyclopropane-Exatecan participated in the formation of the ADC hu2F7-Exatecan (compound 34), which showed antitumor activity in vivo and in vitro. |
