irinotecan

Irinotecan (CPT-11), a derivative of camptothecin, is an inhibitor of DNA topoisomerase I (Topo I). Irinotecan has antitumor activity by preventing DNA strand reattachment through binding to the Topo I complex, resulting in double-stranded DNA breaks and cell death.

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.

Irinotecan hydrochloride trihydrate (CPT-11 HCl Trihydrate) keeps DNA from unwinding by inhibiting topoisomerase 1.

Irinotecan Carboxylate Sodium Salt is a DNA topoisomerase inhibitor.

Irinotecan-d10 Hydrochloride is a deuterated compound of Irinotecan Hydrochloride. Irinotecan Hydrochloride has a CAS number of 100286-90-6. Irinotecan 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.

Irinotecan Impurity 52-d5 is a deuterated compound of Irinotecan Impurity 52.Irinotecan Impurity 52 has a CAS number of 1026078-50-1.

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.

NMac1 (Nm23 activator 1) is a natural compound, cassumunene, derived from Zingiber cassumunar Roxb. and traditionally used as an anti-inflammatory agent in East Asia. NMac1 exhibits anti-metastatic potential by directly interacting with the C-terminal of Nm23-H1, activating its NDP kinase (NDPK) enzymatic activity in vitro. NMac1 inhibits breast cancer metastasis in vivo.

RPR121056 is a Irinotecan metabolite, which is generated by CYP3A4. Irinotecan is an antineoplastic agent that inhibits topoisomerase type I.

Compound LE-77, known as FXR CES2 modulator 1, functions as a dual regulator that activates FXR and inhibits CES2. It effectively mitigates the intestinal toxicity of irinotecan.

Top HDAC-IN-3 (Compound 31) is a dual inhibitor of Topoisomerase and HDAC with oral activity. It induces DNA damage by elevating reactive oxygen species (ROS) levels, consequently inhibiting the clonal formation and migration of cancer cells, and triggering apoptosis (Apoptosis) and cell cycle arrest. Top HDAC-IN-3 demonstrates a significant antitumor effect in NSCLC models, exhibiting a tumor growth inhibition (TGI = 77.5%, 100 mg kg) superior to that of the HDAC inhibitor SAHA and the combination of SAHA with the topoisomerase inhibitor Irinotecan.

BGC0222 is a novel Irinotecan prodrug. As a PEG-cRGD conjugated derivative of Irinotecan, BGC0222 enables the slow and steady release of Irinotecan. It binds to the αVβ3 target with an IC50 of 4.25 μM and has an IC50 of 58.7 μM for αVβ5. BGC0222 can induce angiogenesis and demonstrates significant antitumor activity in various tumors.

FOLFIRI Regimen is a chemotherapy regimen consisting of leucovorin calcium (calcium folinate), 5-fluorouracil, and irinotecan used during the treatment of advanced-stage and metastatic colorectal cancer.

Potent and selective ATM kinase inhibitor (IC50 = 0.6 nM in an enzyme inhibition assay). Exhibits > 600-fold selectivity for ATM over other kinases. Inhibits ATM kinase in an in vitro cellular assay (IC50 = 0.33 μM). Potentiates the antitumor effects of the topoisomerase 1 inhibitor irinotecan in tumor bearing, immunocompromised mice. Orally bioavailable. Degorce et al (2016) Discovery of novel 3-quinoline carboxamides as potent, selective and orally bioavailable inhibitors of ataxia telangiectasia mutated (ATM) kinase. J.Med.Chem. 59 6281 PMID:27259031

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.

1. Biotransformation of glucoAurantio-obtusin towards Aurantio-obtusin increased the toxicity of irinotecan through increased inhibition of SN-38 glucuronidation. 2. Aurantio-obtusin, stimulated chemotactic migration of MC3T3-E1 osteoblast cells in a conc

AZ1366 is a potent tankyrase inhibitor that enhances irinotecan activity in tumors that exhibit elevated tankyrase and irinotecan resistance. Combination AZ1366 and irinotecan achieved greater anti-tumor effects compared to monotherapy. Activity was limited to CRC explants that displayed irinotecan resistance and increased protein levels of tankyrase and NuMA.

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].

Antitumor agent-61 (Compound 9b), an Irinotecan (Ir) derivative, demonstrates potent anticancer activity with IC50 values ranging from 0.92 to 3.23 μM against six human cancer cell lines: SK-OV-3, SK-OV-3 CDDP, U2OS, MCF-7, A549, and MG-63, and specifically induces apoptosis in SK-OV-3 cells via mitochondrial pathways [1].

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].

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].

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].

Compound 44 (hCES2A-IN-2) is an orally active inhibitor of human carboxylesterase 2 (hCES2A) with an IC50 of 5.02 μM, which ameliorates Irinotecan-induced delayed diarrhea [1].