ADC Cytotoxin

Dolastatin 15 originally isolated from the sea hare Dolabella auricularia belongs to a family of antimitotic and antineoplastic depsipeptides inducing apoptosis in various malignant cell types. It was shown to inhibit the growth of the P388 lymphocytic leukemia cell line efficiently, with an ED?? value of 2.4 ng/mL.

MMAF is a potent inhibitor of tubulin polymerization. MMAF works by blocking the process of tubulin polymerization, disrupting the intracellular microtubule network, thereby inhibiting cell division and inducing apoptosis.

Daunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent anti-tumor activity.

Methotrexate is an antifolate antimetabolite that effectively inhibits the activity of dihydrofolate reductase (DHFR), with an IC 50 of approximately 7nM.

A microtubule depolymerizing agent

Paclitaxel (Taxol) is a microtubule-stabilizing agent that exhibit scytotoxic effects against a broad range of tumors.

Daunorubicin is a natural anthracycline antibiotic that intercalates into DNA double strands and inhibits topoisomerase II activity, thereby blocking DNA replication and transcription and inducing tumor cell apoptosis.

Aldoxorubicin, an albumin-binding prodrug of doxorubicin (DNA topoisomerase II inhibitor), is released from albumin under acidic conditions.

Antitumor agent

Monomethyl auristatin E is a potent synthetic microtubule inhibitor derived from dolastatin 10, commonly used as the toxic payload in antibody-drug conjugates (ADCs).

Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent.

Calicheamicin is a cytotoxic agent that causes double-strand DNA breaks.

Mertansine is a potent microtubule-targeted compound that inhibits tubulin assembly into microtubules, with the K D value of 0.86μM.

Duocarmycin TM is a highly potent synthetic DNA minor-groove-binding alkylating antitumor antibiotic that induces sequence-selective alkylation of double-stranded DNA.

Taltobulin (HTI-286) (HTI-286), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin (HTI-286) inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.

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

DXd is a derivative of Exatecan (DX-8951).

PF-06380101 (Aur0101), an auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue. PF-06380101 (Aur0101) shows excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.

Tubulysin A (TubA)(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.

SJG-136 (NSC-694501) is a DNA cross-linking agent, with an XL50 of 45 nM for pBR322 DNA. SJG-136 (NSC-694501) has potent antitumor activity.

Taltobulin trifluoroacetate (HTI-286 trifluoroacetate) (HTI-286 trifluoroacetate), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin trifluoroacetate (HTI-286 trifluoroacetate) inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.

DC1, an analogue of the minor groove-binding DNA alkylator CC-1065, is a ADC Cytotoxin. DC1 can be used in synthesis of antibody-drug conjugates for the targeted treatment of cancer.