ADC Cytotoxin

Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.

Doxorubicin hydrochloride (Adriamycin) belongs to the anthracycline class of antibiotics and is an inhibitor of human DNA topoisomerase I II (IC50=0.8 2.67 μM). Doxorubicin hydrochloride exhibits cytotoxicity and antitumor activity. Doxorubicin hydrochloride reduces the phosphorylation of AMPK and its downstream target protein acetyl coenzyme A carboxylase, and induces apoptosis and autophagy.

Duocarmycin TM is a DNA alkylator. Duocarmycin TM is an exceptionally potent antitumor antibiotic.

Mertansine is a tubulin inhibitor and an antibody-conjugable maytansinoid alkaloid. The IC50 of Mertansine against HCT-15 and A431 cells is 0.750 and 0.04nM.

Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist and IL receptor modulator with anti-inflammatory and immunosuppressive properties that induces autophagy and inhibits LPS-induced inflammatory responses in macrophages.

Dxd (OQM5SD32BQ) is a potent inhibitor of DNA topoisomerase I with an IC50 of 0.31 μM. It is used as a conjugated drug of HER2-targeting ADC.

Exatecan (DX-8951f) is a DNA topoisomerase I (TOP1) inhibitor with an IC50 value of 2.2 μM (0.975 μg mL).Exatecan has antitumor activity and may be used in cancer research.

Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive activities, and is commonly used in rheumatoid arthritis and various tumors.

Calicheamicin (Calicheamicin γ1) is an antitumor antibiotic and is a DNA synthesis inhibitor. It also is a cytotoxic agent that causes double-strand DNA breaks.

Eribulin (B1939) is a nonpaclitaxel microtubule kinetic inhibitor with anticancer activity that inhibits polymerization of microtubule protein subunits by preventing lengthening and shortening of microtubules during cell division.Eribulin is used in the study of metastatic breast cancer and solid tumors.

Daunorubicin hydrochloride (Rubidomycin hydrochloride), an anthracycline aminoglycoside antineoplastic, inhibits DNA replication and repair and RNA and protein synthesis.

10-Methoxycamptothecin, a natural bioactive derivative of camptothecin (CPT) isolated from *Camptotheca acuminata*, exhibits potent anti-cancer properties.

Monomethyl auristatin E (MMAE) (MMAE), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin and also has inhibition of antibody-drug conjugates (ADCs) activity.

MMAF (MonoMethyl auristatin F), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin.

17-AEP-GA is an HSP90 antagonist, a potent inhibitor of glioblastoma cell proliferation, survival, migration, and invasion, and a toxic component of antibody-coupled activated molecules (ADCs), which can be used to study glioblastomas.

Dolastatin 10 (DLS 10) is a potent peptide with antimitotic properties, effectively inhibiting tubulin polymerization.

alpha-Amanitin (alpha-Amanitin) is the lethal toxin in Trichoderma viride and acts in vivo via the enterohepatic circulation and transport system. alpha-Amanitin induces cell death and can be used in the synthesis of ADCs. alpha-Amanitin has been shown to induce cell death and can be used in the synthesis of ADCs.

DM4 (Ravtansine) can be used in the preparation of antibody drug conjugate and it is an antitubulin agent. It can inhibit cell division.

7-Epi 10-desacetyl paclitaxel (10-Deacetyl-7-epipaclitaxel) shows IC50 values of 0.085 nM, against HeLa cells.

Fluticasone propionate (CCI-187881), derived from fluticasone used to remedy asthma and allergic rhinitis, is a high affinity, selective GR (glucocorticoid receptor) agonist.

Glucocorticoid receptor agonist-1, a potent glucocorticoid receptor agonist, has an IC50 of 2.8 nM[1].

Methotrexate disodium is an tetrahydrofolate dehydrogenase inhibitor

Exatecan Mesylate (DX8951f) is a DNA topoisomerase I inhibitor (IC50: 2.2 μM, 0.975 μg mL).

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 = 650 nM). It inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome, displaying low-nM to sub-nM IC50s. Thailanstatin A, as a payload for ADCs, is conjugated to the lysines on trastuzumab, yielding linker-less ADC.

(4-NH2)-Exatecan is a topoisomerase inhibitor with potential anticancer activity for the synthesis of antibody drug conjugates (ADCs).

Budesonide (Pulmicort), an anti-inflammatory corticosteroid, has shown the effective glucocorticoid activitie and few mineralocorticoid activities. According to reports, Budesonide has extensively inhibitory effects against multiple cells types and mediators referred to allergic and nonallergic-mediated inflammatory. What's more, the anti-inflammatory action of budesonide has been revealed to contribute to the effectiveness of asthma.

PNU-159682, a metabolite of anthracycline neomycin, is a DNA topoisomerase II inhibitor with excellent cytotoxicity.

MMAD (Demethyldolastatin 10) is a potent tubulin inhibitor. MMAD is a toxin payload in antibody drug conjugates (ADCs).

DM1-SMe (DM1-SSMe) is a potent inhibitor of maytansinoid microtubular. DM1-SMe is about 3 to 10-fold more potent than the parent drug Maytansine, with IC50s of 0.003 to 0.01 nM for DM1-SMe in a panel of human tumor cell lines.

Auristatin E, a cytotoxic tubulin modifier, disrupts cell division by inhibiting tubulin polymerisation. This compound demonstrates potent and selective antitumor activities, serving as an MMAE analog and cytotoxin in antibody-drug conjugates.

Auristatin F is an effective inhibitor of microtubule and vascular damaging agent. Auristatin F can be used in antibody-drug conjugates.

10-Deacetyl-7-xylosyl paclitaxel (7-Xylosyl-10-deacetyltaxol) is a Paclitaxel derivative with improved pharmacological features and higher water solubility,used in Chinese clinics to treat cancer.

Maytansinol (Ansamitocin P-0) inhibits microtubule assembly and causes microtubule disassembly in vitro.

MMAF-OMe (Monomethyl auristatin F methyl ester) is an antitubulin agent which inhibits several tumor cell lines with IC50s of 0.056 nM, 0.166 nM, 0.183 nM, and 0.449 nM for MDAMB435 5T4, MDAMB361DYT2, MDAMB468, and Raji (5T4-) cell lines, respectively. MMAF-Ome is also an ADC cytotoxin.

(S)-Seco-Duocarmycin SA is a DNA alkylating agent and antibiotic with potent antitumor activity that can be used to synthesize ADC compounds.

AXC-666 is a TLR agonist and an immuno agonist that can be used to synthesize antibody drug couplers (ADCs).

FL118-14-Propanol is a cytotoxic camptothecin derivative, a potential topoisomerase I inhibitor with potential antitumor activity, which can be used in the synthesis of ADC compounds.

Duostatin 5 (Duo-5) is a sea hare toxin analog commonly used in the synthesis of ADC compounds.

SGD-1882 (PBD dimer) is a cytotoxic conjugate that is a target for mouse and human hematopoietic stem cells (HSC) and acute myeloid leukemia cells.

Aldoxorubicin has effective antitumor activities in various cancer cell lines and in murine tumor models. Aldoxorubicin is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitors).

SG2057 (DRG16), a potent antitumor agent, is a pyrrolobenzodiazepine (PBD) dimer connected by a pentyldioxy linkage. This compound selectively binds to the minor groove of DNA, forming both interstrand and intrastrand cross-linked adducts, contributing to its high antitumor activity.

Taltobulin (HTI-286) is a synthetic analog of the tripeptide cysteine, a microtubule protein inhibitor that inhibits liver tumor cell proliferation in vitro and tumor growth in vivo.Taltobulin is cytotoxic, induces mitotic arrest and apoptosis, and may be used in the study of breast cancer and microtubule tissue-related diseases.

(rac)-Exatecan Intermediate 1 is a camptothecin derivative, a potential topoisomerase I inhibitor, used in tumor research.

Taltobulin trifluoroacetate is a synthetic analogue of the tripeptide hemiasterlin, is a potent agent of antimicrotubule that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.

Doxorubicin (Adriamycin) is a Topoisomerase II (Top2) inhibitor with antineoplastic activity.

Tubulysin E is a natural product isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis, and is a highly cytotoxic peptide.

PNU-159682 carboxylic acid is a potent ADCs cytotoxin,PNU-159682 carboxylic acid has protein fold and diverse functions.

Corixetan is a potent thorium chelator that effectively forms stable complexes with Th-227 in vivo.