sn38

SN-38 (NK012) is the active metabolite of Irinotecan, a DNA topoisomerase I (Topo I) inhibitor, which inhibits DNA and RNA synthesis (IC50=0.077 1.3 μM). SN-38 has antitumor activity and induces autophagy.

MC-VC-PAB-DMEA-SN38 is a thiol-reactive Drug-linker, featuring an innovative highly stable and degradable linker. SN-38 can inhibit the synthesis of DNA and RNA, and is commonly used in the synthesis of antibody-drug conjugates (ADC).

NH2-PEG4-VC-PAB-DMEA-SN38 is a transpeptidase reaction-type Drug-linker with an innovative highly stable and degradable linker. SN38 can inhibit the synthesis of DNA and RNA, and can be used in the synthesis of antibody-drug conjugates (ADCs).

CL2-MMT-SN38 is a derivative of SN-38, which is a potent anticancer agent and the active metabolite of Irinotecan (CPT-11), a Topoisomerase I inhibitor.

MC-SN38 is a drug-linker conjugate that pairs the potent microtubule-disrupting agent SN38 with a non-cleavable MC linker, designed for use in antibody drug conjugates (ADCs). SN38, the active metabolite of the Topoisomerase I inhibitor Irinotecan, works by inhibiting DNA synthesis and inducing DNA single-strand breaks.

Mc-VC-PAB-SN38 consists of a cleavable ADC linker (Mc-VC-PAB) and SN38, which is part of an antibody-coupled reactive molecule commonly used to synthesize antibody-coupled reactive molecules (ADCs) that target sites of action.

SN38-COOH, the active metabolite of the topoisomerase I inhibitor irinotecan, is utilized in the synthesis of antibody-drug conjugates (ADCs). It functions by inhibiting DNA and RNA synthesis [1] [2].

SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3 is a drug-linker conjugate for antibody-drug conjugates (ADCs), consisting of the anti-cancer agent SN38 linked to Lys(MMT)-PAB-oxydiacetamide-PEG8-N3. It serves as a click chemistry reagent featuring an azide group that participates in copper-catalyzed azide-alkyne cycloaddition (CuAAC) with alkyne-bearing molecules and can also engage in strain-promoted alkyne-azide cycloaddition (SPAAC) with compounds containing DBCO or BCN groups, facilitating the synthesis of ADCs [1].

Mal-va-mac-SN38 is a conjugate molecule functioning as an ADC (Antibody-Drug Conjugate) drug-linker. This compound comprises the cytotoxic ADC agent SN-38 and a linker. Once inside the body, Mal-va-mac-SN38 rapidly forms a covalent bond with endogenous albumin, resulting in the formation of HSA-va-mac-SN38. It demonstrates remarkable stability in human plasma and exhibits both antitumor and antimetastatic properties.

CL2E-SN-38 TFA, a structurally stable and highly releasable antibody drug conjugate (ADC), comprises SN-38, the active metabolite of Irinotecan derived from camptothecins, known for its Topoisomerase I inhibitory activity [1].

CL2E-SN-38 is a structurally stable and highly releasable antibody-drug conjugate (ADC) incorporating SN-38, the active metabolite of Irinotecan and a potent Topoisomerase I inhibitor [1] from the camptothecins class.

CL2A-SN-38 consists of a CL2A linker and an anticancer compound, SN-38, which delivers active molecules within tumor cells and in the tumor microenvironment, often in conjunction with antibodies to make biologically active antibody-coupled reactive molecules (ADCs).

TP3011 is a potent topoisomerase I inhibitor equipotent as SN38 and is an active metabolite of CH-0793076.

MAC glucuronide phenol-linked SN-38, a pH-sensitive lactone and DNA topoisomerase I inhibitor drug linker, exhibits cytotoxicity in L540cy and Ramos cells, with IC50 values of 113 ng mL and 67 ng mL, respectively[1].

MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a cytotoxic drug linker that maintains a stabilized lactone form, demonstrating efficacy against L540cy and Ramos cells with IC50 values of 99 and 105 ng mL, respectively[1].

CLM3, a pyrazolopyrimidine derivative, functions as a multitargeted tyrosine kinase inhibitor. It exhibits antiproliferative and proapoptotic activities on endothelial and cancer cells, activities that are synergistically enhanced by SN38. The primary mechanism of action for CLM3 involves the inhibition of phosphorylation in tyrosine kinases such as VEGFR-2, EGFR, and RET, along with their associated signaling pathways.

DTS-108 is a prodrug of SN38 (a topoisomerase I inhibitor). It is a conjugate formed by linking SN38 to a human oligopeptide through an esterase-sensitive crosslinker. DTS-108 exhibits anticancer activity against colorectal cancer, lung cancer, and breast cancer.

SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol L on the isolated human enzyme.

Labetuzumab govitecan is an anti-CEACAM5 SN-38 antibody-drug conjugate for therapy of refractory or relapsing metastatic colorectal cancer.

Ki23057 is a a FGFR2 inhibitor, which enhances the chemosensitivity of drug-resistant gastric cancer cell lines when used in combination with chemotherapeutic drugs. Ki23057 might be therapeutically promising for treating drug-resistant gastric cancer cells, especially when used in combination with SN38, PTX, or VP16. The apoptosis process might be the main mechanism underlying the synergistic effect of these combinations. The ERCC1 and p53 genes may play an integral role in the synergism between Ki23057 and chemotherapeutic agents in drug-resistant cell lines. (source: Cancer Lett. 2011 Aug 1;307(1):47-52).

ZBH-1205 is a novel camptothecin derivative, revealing potent antitumor activities mainly through cell apoptosis pathway, being more effective than cpt-11 and sn38 at inhibiting topoismerase-1

Antitumor Agent-102 (Compound 10), a conjugate integrating a Topoisomerase I inhibitor SN38 with a glucose transporter inhibitor, specifically targets colorectal cancer. This agent facilitates elevated levels of free SN38 in tumor tissues compared to Irinotecan [1].

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.