Traditional Cytotoxic Agents
Traditional cytotoxic agents inhibit cancer cell proliferation by disrupting macromolecular synthesis, DNA integrity, and mitotic progression, leading to direct cytotoxicity or apoptosis[1]. Mechanistically, alkylating agents induce DNA damage, antimetabolites interfere with DNA/RNA synthesis, topoisomerase inhibitors block DNA replication, and antimicrotubule agents impair mitosis[2]. These pathways remain relevant in oncology because cytotoxic chemotherapy acts on pan-essential cellular processes, while response depends on cell-intrinsic mechanisms and the tumor microenvironment[2][3]. Compared with targeted agents, traditional cytotoxic agents show limited tumor selectivity because DNA damage and protein-expression disruption also affect normal host cells[1][4]. Within this class, topoisomerase I and II inhibitors differ from taxanes and vinca alkaloids because they target DNA-processing enzymes, whereas microtubule agents regulate spindle dynamics and metaphase progression[1][5]. For experimental applications, these inhibitors provide practical tools to model DNA damage response, mitotic arrest, apoptosis, resistance, and chemotherapy-sensitive tumor microenvironments[2][4][5].
References:
- [1]. Amjad MT, et al. Cancer Chemotherapy. 2023 Feb 27. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2026 Jan–. [Content Brief]
- [2]. Tilsed CM, et al. Cancer chemotherapy: insights into cellular and tumor microenvironmental mechanisms of action. Front Oncol. 2022 Jul 29;12:960317. [Content Brief]
- [3]. Rudd SG. Targeting pan-essential pathways in cancer with cytotoxic chemotherapy: challenges and opportunities. Cancer Chemother Pharmacol. 2023 Oct;92(4):241-251. doi: 10.1007/s00280-023-04562-3. Epub 2023 Jul 15. PMID: 37452860; PMCID: PMC10435635. et al. Targeting pan-essential pathways in cancer with cytotoxic chemotherapy: challenges and opportunities. Cancer Chemother Pharmacol. 2023 Oct;92(4):241-251. [Content Brief]
- [4]. van den Boogaard WMC, et al. Chemotherapy Side-Effects: Not All DNA Damage Is Equal. Cancers (Basel). 2022 Jan 26;14(3):627. [Content Brief]
- [5]. Jordan MA, et al. Microtubules as a target for anticancer drugs. Nat Rev Cancer. 2004 Apr;4(4):253-65. [Content Brief]
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Traditional Cytotoxic Agents Related Products (24)
Related Products (24)
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α-Amanitin
0 ImagesCat. No.: HY-19610CAS No.: 23109-05-9Synonyms: α-Amatoxinα-Amanitin is the principal toxin of several deadly poisonous mushrooms, exerting its toxic function by inhibiting RNA-polymerase II.
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β-Amanitin
0 ImagesCat. No.: HY-125586CAS No.: 21150-22-1β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
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γ-Amanitin
0 ImagesCat. No.: HY-131081CAS No.: 21150-23-2γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNA polymerase II and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin and β-Amanitin. γ-Amanitin competitively binds to monoclonal antibody (mAb), with an IC50 of 163.1 ng/mL. γ-Amanitin is toxic to a variety of cells.
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Taltobulin
0 ImagesSynonyms: HTI-286; SPA-110Taltobulin (HTI-286), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
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Tubulysin A
0 ImagesSynonyms: TubATubulysin A (TubA) is an anticancer and antiangiogenic agent with anti-microtubule, anti-mitosis and anti-proliferative activity against a variety of cancer cells with IC50 values in the pmol range. It can induce apoptosis of cancer cells and has no effect on normal cells. Tubulysins are a group of potent cytotoxins consisting of nine members (A-I). Tubulysin A can synthesize ADC as ADC Cytotoxin.
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Glucocorticoid receptor agonist-5
0 ImagesGlucocorticoid receptor agonist-5 (compound 4), a glucocorticoid molecule, is a potent glucocorticoid receptor agonist. Glucocorticoid receptor agonist-5 shows anti-inflammatory and immunosuppressive activity. Glucocorticoid receptor agonist-5 is used as an ADC Cytotoxin for antibody-drug conjugate.
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10-Deacetyl-7-xylosyl paclitaxel
0 ImagesSynonyms: 10-Deacetyl-7-xylosyltaxol; 10-Deacetylpaclitaxel 7-Xyloside; 10-Deacetyltaxol 7-Xyloside10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel (a microtubule stabilizing agent; enhances tubulin polymerization) derivative with improved pharmacological features.
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Taltobulin hydrochloride
0 ImagesCat. No.: HY-15584BPurity: 99.34%Synonyms: HTI-286 hydrochloride; SPA-110 hydrochlorideTaltobulin hydrochloride (HTI-286 hydrochloride), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin hydrochloride inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
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Taltobulin trifluoroacetate
0 ImagesCat. No.: HY-15584ACAS No.: 228266-41-9Synonyms: HTI-286 trifluoroacetate; SPA-110 trifluoroacetateTaltobulin trifluoroacetate (HTI-286 trifluoroacetate), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin trifluoroacetate inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
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C-11
0 ImagesCat. No.: HY-100861CAS No.: 2007965-97-9C-11 is a tubulin inhibitor and acts as an ADC cytotoxin, displays cytotoxicity for carcinoma cell lines.
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Rebeccamycin
0 ImagesCat. No.: HY-19825CAS No.: 93908-02-2Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II.
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Isofistularin-3
0 ImagesCat. No.: HY-19826Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.
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ε-Amanitin
0 ImagesCat. No.: HY-131083CAS No.: 21705-02-2ε-Amanitin, a cyclic peptide isolated from a variety of mushroom species, potently binds to and inhibits the activity of RNA polymerase II.
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Mensacarcin
0 ImagesCat. No.: HY-122534CAS No.: 808750-39-2Mensacarcin, a highly complex polyketide, strongly inhibits cell growth universally in cancer cell lines and potently induces apoptosis in melanoma cells. Mensacarcin targets to mitochondria, affects energy metabolism in mitochondria, and activates caspase-dependent apoptotic pathways. Mensacarcin, an antibiotic, can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
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Tubulysin IM-2
0 ImagesCat. No.: HY-130959CAS No.: 1032072-50-6Tubulysin IM-2 is a microtubule/Tubulin inhibitor that can act as an ADC cytotoxin (ADC Cytotoxin) and an anti-microtubule toxin (anti-microtubule toxins). Used for ADC synthesis.
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Tubulysin IM-3
0 ImagesCat. No.: HY-130960CAS No.: 1639986-05-2Tubulysin IM-3 is a microtubule/Tubulin inhibitor that can act as an ADC cytotoxin (ADC Cytotoxin) and an anti-microtubule toxin (anti-microtubule toxins). Used for ADC synthesis.
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17-AEP-GA
0 ImagesCat. No.: HY-133570CAS No.: 75747-23-817-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin.
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Polyketomycin
0 ImagesCat. No.: HY-106338CAS No.: 200625-47-4Polyketomycin is a tetracyclic quinone glycoside antibiotic isolated from Streptomyces sp. or Streptomyces diastatochromogenes. Polyketomycin inhibits growth of Gram-positive bacteria, and its MIC values is less than 0.2 µg/mL. Polyketomycin has antibacterial, anticancer, antimalarial activities.
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Azonafide-PEABA
0 ImagesCat. No.: HY-126664CAS No.: 2752193-52-3Azonafide-PEABA is a cytotoxic agent moiety.
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