Paclitaxel is a potent anticancer medication which can promote microtubule (MT) assembly, inhibit MT depolymerization, and change MT dynamics required for mitosis and cell proliferation.
Tubulysin A(TubA) is a myxobacterial product that can function as an antiangiogenic agent in many in vitro assays; anti-microtubule, anti-mitotic, an apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative.IC50 value: Target: microtubuleTubulysin A is a novel antibiotic, which is anti-microtubule, anti-mitotic, apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative. Tubulysins are cytotoxic peptides, which include 9 members (A-I). Tubulysin A has potential application as an anticancer agent. It arrests cells in the G2/M phase. Tubulysin A inhibits polymerization more efficiently than vinblastine and induces depolymerization of isolated microtubules. Tubulysin A has potent cytostatic effects on various tumor cell lines with IC50 in the picomolar range.
SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent[1].
Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
DM1-SMe is an unconjugated form of the Maytansinoid in IMGN901. DM1-SMe is about 3-10-fold more potent than the parent drug Maytansine, with IC50s ranging from 0.003 to 0.01 nM for DM1-SMe in a panel of human tumor cell lines[1].
Py-MPB-amino-C3-PBD is a cytotoxic agent comprised non-alkylating group. Py-MPB-amino-C3-PBD acts as the payload for ADCs. Antimicrobial activity[1].
MMAF hydrochloride is an antitubulin agent that inhibit cell division; inhibits H3397 cell growth with an IC50 of 105 nM.
Doxorubicin hydrochloride is a cytotoxic anthracycline antibiotic for the treatment of multiple cancers. The possible mechanisms by which doxorubicin acts in the cancer cell are intercalation into DNA and disruption of topoisomerase-II-mediated DNA repair.
ε-Amanitin, a cyclic peptide isolated from a variety of mushroom species, potently binds to and inhibits the activity of RNA polymerase II[1][2].
Maytansinoid B is a kind of ADC Cytotoxin. Maytansinoid B can be used to conjugates with antibodies to form Antibody-Drug Conjugates (ADCs). Maytansinoids are known as antimitotic agents, binding to tubulin and inhibiting microtubule assembly. Maytansinoids induces G2/M arrest in the cell cycle to induce apoptosis[1][2].
Fmoc-MMAF-OMe is an anticancer agent and tubulin polymerization inhibitor with an Fmoc protecting group. The active ingredient of Fmoc-MMAF-OMe, MMAF (HY-15579), is the cytotoxic (ADC Cytotoxin) component of classic antibody drug conjugates (ADCs)[1].
DMEA-PNU-159682 (molecule D12) dichloroacetate is an ADC cytotoxin molecule including metabolites of nemorubicin (MMDX) from liver microsomes and a potent ADCs cytotoxin PNU-159682[1][2].
Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II[1][2].
Mensacarcin, a highly complex polyketide, strongly inhibits cell growth universally in cancer cell lines and potently induces apoptosis in melanoma cells. Mensacarcin targets to mitochondria, affects energy metabolism in mitochondria, and activates caspase-dependent apoptotic pathways. Mensacarcin, an antibiotic, can be used as a cytotoxic component of antibody-drug conjugates (ADCs)[1][2].
Daunorubicin hydrochloride is a topoisomerase II inhibitor with potent antineoplastic activities.
Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers[1][2].
SGD-1882 is a cytotoxic, DNA minor-groove crosslinking agent pyrrolobenzodiazepine (PBD) dimer, acting as the payload for ADCs.
N-Boc-Val-Dil-Dap-Doe is a compound used to synthesize Dolastatin 10. Dolastatin 10, a potent antimitotic peptide, inhibits tubulin polymerization[1].
Inebilizumab is an anti-CD19 monoclonal antibody (mAb) with enhanced antibody-dependent cell-mediated cytotoxicity against B cells. Inebilizumab can be used for multiple sclerosis and neuromyelitis optica research[1].
ADC toxin 1 is an ADC cytotoxin with anti-cancer activities. ADC toxin 1 is against HCT-116 and PSN1 cells growth with both IC50 values of 0.86 µM.
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivative with improved pharmacological features and higher water solubility.IC50 value:Target: Microtubule inhibitor10-Deacetyl-7-xylosyl paclitaxel induced mitotic cell cycle arrest and apoptosis as measured by flow cytometry, DNA laddering, and transmission electron microscopy. Pro-apoptotic Bax and Bad protein expression was up-regulated and anti-apoptotic Bcl-2 and Bcl-XL expression down-regulated, which lead to a disturbance of the mitochondrial membrane permeability and to the activation of caspase-9. In turn, caspase-9 activated downstream caspases-3 and -6, but not caspase-8. Bid was also activated by caspase-3. Reversely, treatment with a caspase-10-specific inhibitor could not protect PC-3 cells from 7-xylosyl-10-deacetyl-paclitaxel-triggered apoptosis. Moreover, 7-xylosyl-10-deacetylpaclitaxel had no effect on the expression of CD95 and NF-kappaB proteins, indicating that apoptosis was induced through the mitochondrial-dependent pathway in PC-3 cells.
Exatecan-methylacetamide-OH (compound 6) is a Exatecan derivative with anticancer effects. Exatecan-methylacetamide-OH is an ADC cytotoxin that can be used to synthesize Antibody-Drug Conjugates (ADCs) (CN112125915A; compound 6)[1].
NH2-methylpropanamide-Exatecan TFA is a methylpropanamide-modified Exatecan (HY-13631), which is the common ADC Cytotoxin used in the synthesis of ADC. Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research[1].
Exatecan Mesylate is a water soluble topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
Luisol A, an aromatic tetraol, is a major metabolite of an estuarine marine actinomycete of the genus Streptomyces. Luisol A, anthraquinone antibiotic analog, is an ADC Cytotoxin[1].
Ansamitocin P-3 is a microtubule inhibitor. Ansamitocin P-3 is a macrocyclic antitumor antibiotic.
MC-DOXHZN hydrochloride is an albumin-binding prodrug of Doxorubicin, with acid-sensitive properties[1].
Methotrexate-d3 (Amethopterin-d3) is the deuterium labeled Methotrexate. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].
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[1][2][3].
Seco-DUBA hydrochloride is a toxin for ADC drug SYD985[1].