camptothecin

Camptothecin (CPT) belongs to the alkaloid group of natural products and is a specific DNA topoisomerase I (Topo I) inhibitor (IC50=679 nM) with specificity. Camptothecin has antitumor activity and induces apoptosis.

CZ-48 is a DNA topoisomerase inhibitor.

MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin (compound 21a) is a camptothecin payload used in the synthesis of a camptothecin antibody-drug conjugate (ADC) by conjugating it to a monoclonal antibody (mAb).

Camptothecin-20(S)-O-propionate hydrate, the C20-propionate ester of CPT, serves as a potent anticancer agent and functions as a topoisomerase-I inhibitor [1] [2]. This compound is often referenced by its alternate name, Camptothecin-20-O-propionate.

Sodium Camptothecin is a plant alkaloid with antitumor activity. Sodium Camptothecin is a reversible RNA synthesis inhibitor. Sodium Camptothecin is an effective adenovirus replication inhibitor. Sodium Camptothecin inhibits DNA synthesis and causes breaks in intracellular preformed viral DNA.

12-Ethyl-9-hydroxycamptothecin (SN38) is the active metabolite of irinotecan, a topoisomerase I inhibitor, with potential anticancer activity for use in the study of colon and rectal cancer.

Irinotecan Hydrochloride (CPT-11 hydrochloride) is the hydrochloride salt of a semisynthetic derivative of camptothecin. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent.

9-amino-CPT (Aminocamptothecin) is an inhibitor of topoisomerase I with potent anticancer activity.

Calphostin I is isolated from the fungus Cladosporium cladosporioides and is an inhibitor of protein kinase C (PKC).

FL118 is a novel survivin inhibitor that inhibits cancer stem cell-like properties.FL118 is a novel camptothecin analog with anticancer activity that inhibits epithelial-mesenchymal transition through the Wnt/β-catenin signaling pathway, thereby inhibiting migration and invasion of human breast cancer cells.

(5R)-Dimethylbenzene-camptothecin (Compound 6a) is a derivative of camptothecin. It exhibits cytotoxic effects on tumor cells and can induce apoptosis and cell cycle arrest. Additionally, (5R)-Dimethylbenzene-camptothecin demonstrates antitumor activity.

Camptothecin derivative-3 (Compound 11) is a camptothecin derivative utilized as a payload for ADCs. It exhibits cytotoxic properties with IC50 values of 2 nM for HSC-2 and 0.9 nM for Namalwa/luc. Camptothecin derivative-3 is applicable in tumor-related research.

7-Methylol-9-methoxy-10-F-camptothecin (Compound D6-1) is a derivative of Camptothecin. This compound can serve as a cytotoxic payload for synthesizing antibody-drug conjugates (ADCs).

MC-GGFG-AM-(10Me-11F-Camptothecin) serves as a linker-payload conjugate in the synthesis of ZW251, an antibody-drug conjugate (ADC) targeting human GPC3. ZW251 comprises a humanized IgG1 antibody linked to ZD06519, a novel camptothecin-based topoisomerase 1 inhibitor, through a maleimide-anchor and a cleavable glycyl glycyl phenylalanyl glycine (GGFG)-aminomethyl (AM) linker. ZW251 demonstrates strong affinity for GPC3 in both human and cynomolgus monkey cells, characterized by rapid internalization in GPC3-positive Hepatocellular Carcinoma (HCC) cell lines and induces bystander-mediated killing of GPC3-negative cancer cells [1].

7-Aminomethyl-10-methyl-11-fluoro camptothecin, serving as a cytotoxic component of the antibody-drug conjugate (ADC) MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin, is employed in the synthesis of camptothecin ADCs [1].

9-Chloromethyl-10-hydroxy-11-F-Camptothecin, a novel derivative of camptothecin, functions as a DNA topoisomerase I (Topo I) inhibitor with potential applications in anticancer research [1].

MC-GGFG-AM-(10NH2-11F-Camptothecin) is an antibody-drug conjugate (ADC) that exhibits antitumor activity by targeting TROp-2 with the sacituzumab antibody through a hydrolysable, pH-sensitive linker. It is utilized in cancer research [1].

MC-GGFG-(7ethanol-10NH2-11F-Camptothecin) (compound 141) is a protease-cleavable drug-linker conjugate utilized in antibody-drug conjugates (ADCs), featuring an MC-GGFG linker that allows for enzymatic cleavage [1].

7Ethanol-10NH2-11F-Camptothecin, an antibody drug conjugate (ADC), demonstrates inhibitory effects on tumor growth and is utilized in cancer research [1].

10NH2-11F-Camptothecin, an antibody-drug conjugate (ADC), exhibits antitumor activity and is utilized in cancer research [1].

10NH2-11F-Camptothecin TFA, a Camptothecin analogue, functions as an ADC cytotoxin for antibody-drug conjugates (ADCs) synthesis. It exhibits anticancer properties (WO2022246576A1; compound 140) [1].

7-Aminomethyl-10-methyl-11-fluoro camptothecin TFA, a cytotoxin variant of MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin, is employed in the synthesis of camptothecin antibody-drug conjugates (ADC) [1].

7-Hydroxyethyl carbamate-(10Me-11F-Camptothecin) is an analogue of Camptothecin and serves as an ADC cytotoxin. It is utilized in the synthesis of ADCs and for cancer research [1].

MC-GGFG-AM-(10Me-11F-Camptothecin) intermediate-1 (compound 19-2) serves as a synthetic intermediary for the creation of the drug-linker conjugate, MC-GGFG-AM-(10Me-11F-Camptothecin), utilized in the synthesis of ADCs (Antibody-Drug Conjugates). This intermediate allows for the incorporation of functional groups.