sn-38

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.

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).

CL2-SN-38, a part of the antibody-drug conjugate (ADC), can conjugate with the anti-Trop-2-humanized antibody hRS7. SN-38 is an inhibitor of DNA topoisomerase I.

CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC).. CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a noncleavable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. .

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].

SN-38 glucuronide, an inactive metabolite of Irinotecan, serves as a derivative of this cancer-fighting agent. Irinotecan, known for inhibiting topoisomerase I, is utilized in the research of colon and rectal cancer [1].

SN-38-CM2, a split esterase, achieves over 95% conversion to SN-38 within 5 minutes in vitro and induces protein-protein interactions (PPI)-dependent esterase to mediate cell death in MDA-MB-231 cells [1].

SN-38-d3 is a deuterated form of SN-38. As the active metabolite of the topoisomerase I (TopoisomeraseI) inhibitor irinotecan, SN-38 (NK012) notably inhibits the synthesis of DNA and RNA, with IC50 values of 0.077 and 1.3 μM, respectively.

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

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.

Tacrolimus (FK506, Fujimycin) is a macrolide immunosuppressant that binds to FKBP12 to form a high-affinity complex (Ki = 0.2 nM), which inhibits calcineurin phosphatase activity, thereby suppressing T lymphocyte signal transduction and the transcription and release of IL-2. It exerts potent immunosuppressive effects and can be used to induce immunosuppression models.

CL2 Linker is a cleavableADC linker. CL2-SN-38 and CL2A-SN-38 are equivalent in drug substitution (~6), cell binding (Kd ~1.2 nM), cytotoxicity (IC50 ~2.2 nM), and serum stability in vitro (t1/2 ~20 hours)[1][2].

PROTAC PARP1 degrader-3 (Compound C6) is a PROTAC degrader specifically targeting PARP1, with a DC50 of 58.14 nM. It demonstrates cytotoxicity in SW-620 and LOVO cancer cells, with IC50 values of 1.63 μM and 2.84 μM, respectively. In BRCA-mutated colon cancer cells, PROTAC PARP1 degrader-3 exhibits synergistic effects with SN-38, with a combination index (CI) of 0.487.

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).

Val-Ala-PAB-SN38 is a drug-linker conjugate for ADCs, comprising the ADC linker Val-Ala-PAB and SN38. SN-38 is the active metabolite of irinotecan, which acts as an inhibitor of topoisomerase I (TopoisomeraseI).

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

Delimotecan is a DNA topoisomerase I inhibitor. Delimotecan had a long terminal half-life of 109 h, and relatively high exposures to T-2513 and SN-38 were obtained. The percentage decrease in WBC and absolute neutrophil count significantly correlated with

CAY10719 is a selective inhibitor of the breast cancer resistance protein ABCG2 (IC50 = 0.23 μM) with little activity at ABCG1. It has been shown to reverse the ABCG2-mediated resistance toward SN 38 and to inhibit ATPase activity.

ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s), targeting hGX with an IC50 of 80 nM. It efficiently inhibits the phosphorylation of ERK1/2 and p-38. sPLA2s, part of the disulfide-rich, Ca2+-dependent enzyme family, catalyze the hydrolysis of glycero-phospholipids at the sn-2 position, releasing a fatty acid and a lysophospholipid. ROC-0929 is promising for research on inflammation-related diseases.

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.

YHO-13177 is a potent and specific inhibitor of BCRP, which enhances the cytotoxicity of SN-38 in cancer cells without affecting P-glycoprotein–mediated paclitaxel resistance in [MDR1]-transduced human leukemia [K562] cells.