1. Signaling Pathways
  2. Antibody-drug Conjugate/ADC Related
  3. ADC Cytotoxin
  4. Camptothecins Isoform

Camptothecins

The anti-tumor activity of Camptothecin (CPT) and its derivatives is mainly due to its interaction with Topoisomerase 1 (TOP1), a ubiquitous enzyme involved in the regulation of DNA topology during replication, recombination and transcription. TOP1 forms a phosphotyrosine bond with DNA, catalyzing a forward reaction in which DNA is cleaved to allow unwinding, and a reverse reaction in which DNA is religated. CPT interferes with the religation step of this process by reversibly binding to and stabilizing the enzyme/DNA complex. Once the CPT molecule has intercalated into the TOP1-DNA complex (cleavable complex), the collision between the complex and the replication fork during S-phase is thought to result in DNA double strand breaks (DSBs) that eventually lead to cell death.

Camptothecins Related Products (43):

Cat. No. Product Name Effect Purity
  • HY-13631A
    Exatecan mesylate
    99.98%
    Exatecan mesylate (DX8951f) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research.
  • HY-13631D
    Dxd
    99.30%
    Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).
  • HY-13704
    SN-38
    99.89%
    SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254).
  • HY-16560
    Camptothecin
    99.86%
    Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.
  • HY-13631
    Exatecan
    99.93%
    Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
  • HY-160806
    (5-Cl)-Exatecan
    (5-Cl)-Exatecan (compound 1-5) is a potent DNA topoisomerase inhibitor used in cancer research. (5-Cl)-Exatecan is an ADC Cytotoxin.
  • HY-132162
    7-MAD-MDCPT
    98.00%
    7-MAD-MDCPT, a Camptothecin analog, is a toxin payload in antibody drug conjugates (ADCs).
  • HY-42487
    Exatecan Intermediate 1
    99.99%
    Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan can serve as the cytotoxic component of ADCs, disrupting tumor cell proliferation and division by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers.
  • HY-13631AS
    Exatecan-d5 mesylate
    99.82%
    Exatecan-d5 (mesylate) is deuterium labeled Exatecan mesylate. Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL[1].
  • HY-W021377
    Exatecan Intermediate 2
    99.95%
    Exatecan Intermediate 2 (compound B) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers.
  • HY-145397
    (4-NH2)-Exatecan
    ≥99.0%
    (4-NH2)-Exatecan, a topoisomerase inhibitor, is a derivative of Exatecan. (4-NH2)-Exatecan can be used in the synthesis of antibody-drug conjugates (ADCs) (US20200306243A1, compound A).
  • HY-44369
    Exatecan Intermediate 6
    98.92%
    Exatecan Intermediate 6 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 6 can be used to synthesize Antibody-Drug Conjugates (ADCs).
  • HY-42487B
    (R)-Exatecan Intermediate 1
    99.96%
    (R)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer.
  • HY-156617
    Cyclopropaneacetamide-Exatecan
    Cyclopropaneacetamide-Exatecan (Compound 2-A) is an ADC Cytotoxin and an Exatecan analogue. Cyclopropaneacetamide-Exatecan can be used in the synthesis of ADC such as anti-B7H3 antibody-Exatecan analogue conjugate (compound ADC-2).
  • HY-13631J
    (1R,9R)-Exatecan mesylate
    99.94%
    (1R,9R)-Exatecan mesylate((1R,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNA topoisomerase I with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research.
  • HY-13631AG
    Exatecan mesylate (GMP)
    Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
  • HY-79490
    Ac-Exatecan
    98.70%
    Ac-Exatecan is acetylated Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM).
  • HY-13631I
    (1S,9R)-Exatecan mesylate
    (1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNA topoisomerase I with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research.
  • HY-156617A
    (αR)-Cyclopropaneacetamide-Exatecan
    99.75%
    (αR)-Cyclopropaneacetamide-Exatecan (compound 2-A), an Exenotecan derivative, is a cytotoxic agent. (αR)-Cyclopropaneacetamide-Exatecan inhibits U87MG and SK-BR-3 cells proliferation, with IC50s of 8.11 and 2.31 μM.
  • HY-150401
    Exatecan-amide-cyclopropanol
    98.15%
    Exatecan-amide-cyclopropanol (compound 1) is a anticancer agent. Exatecan-amide-cyclopropanol shows anti-proliferation activity against SK-BR-3 and U87 cells, with IC50 values of 0.12 and 0.23 nM, respectively.