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-D10 (Standard) is a reference standard of Irinotecan-D10 intended for quantitative analysis, quality control, and related biochemical research applications. Irinotecan-d10 is the deuterated form of Irinotecan ((+)-Irinotecan), which acts as an inhibitor of topoisomerase I and is utilized in research related to colon and rectal cancers.

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.

Irinotecan Carboxylate Sodium Salt is a DNA topoisomerase inhibitor.

Irinotecanimpurity 52 is an impurity associated with Irinotecan.

Irinotecan-D10 hydrochloride is a deuterated compound of Irinotecan Hydrochloride. Irinotecan Hydrochloride (T0486L) has a CAS number of 100286-90-6. Irinotecan Hydrochloride (T0486L) 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-D10 is the deuterated form of Irinotecan (T6228) ( (+)-Irinotecan), which acts as an inhibitor of topoisomerase I and is utilized in research related to colon and rectal cancers.

Irinotecan Impurity 52-D5 is a deuterated compound of Irinotecan Impurity 52.Irinotecan Impurity 52 has a CAS number of 1026078-50-1.

Irinotecan (Standard) is a reference standard for research and analysis in studies involving 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-[13C6] (Standard) is a reference standard of Irinotecan-[13C6] intended for quantitative analysis, quality control, and related biochemical research applications.

Irinotecan Impurity 52-D5 (Standard) is a reference standard of Irinotecan Impurity 52-D5 intended for quantitative analysis, quality control, and related biochemical research applications. 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.

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.

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).

hCES2A-IN-2 (compound 14n) is an orally active, highly specific, irreversible, covalent inhibitor of hCES2A with an IC50 of 0.04 nM. It targets and covalently binds to the catalytic serine residue (Ser-228) of hCES2A. hCES2A-IN-2 can significantly mitigate irinotecan-induced gastrointestinal toxicity (ITGT) without diminishing the antitumor efficacy of irinotecan in tumor-bearing mice.

β-Glucuronidase-IN-3 (Compound 49) is a covalent allosteric inhibitor targeting β-glucuronidase. It exhibits potent inhibitory activity against Escherichia coli β-glucuronidase (EcGUS) with an IC50 of 12.9 nM. The compound exerts its inhibitory effect through reversible covalent modification of cysteine residues (Cys28, Cys443, and Cys197) on EcGUS. It is applicable in research on gut microbiota-related diseases, particularly in reducing the toxic side effects of Irinotecan and non-steroidal anti-inflammatory drugs (NSAIDs).

Val-Ala-PAB-SN38 TFA is a drug-linker conjugate for ADCs, composed of the ADC linker Val-Ala-PAB and SN38, which is the active metabolite of the topoisomerase I (Topoisomerase I) inhibitor irinotecan.

MBL-II-141 is a potent ABCG2 inhibitor with an IC50 of 0.11 μM. It inhibits the transport function of ABCG2 in a non-competitive manner, preventing ABCG2 from expelling substrates (such as Irinotecan) out of cells, thereby increasing the intracellular accumulation of the drug. MBL-II-141 does not affect ABCB1 (P-gp) or ABCC1 (MRP1) and exhibits very low cytotoxicity (IG50 > 100 μM). This compound is useful for studying tumor multidrug resistance (MDR).

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.