Cemadotin Hydrochloride (CAS No. 172837-41-1) – Synthetic Anticancer Peptide Analogue

Description

Product Description

Cemadotin hydrochloride (CAS No. 172837-41-1), also known as LU103793, is a water-soluble synthetic analogue of the marine-derived peptide Dolastatin 15. It is a potent inhibitor of tubulin polymerization and cell cycle progression, leading to disruption of mitotic spindle formation and cell cycle arrest at the G2/M phase. Cemadotin hydrochloride has been extensively investigated in preclinical models for its anticancer potential.

Molecular Design and Background
Dolastatin 15, originally isolated from the sea hare Dolabella auricularia, demonstrated powerful cytotoxic effects but limited clinical applicability due to solubility and pharmacokinetic issues. Cemadotin hydrochloride was rationally designed as a more soluble analogue with preserved activity. By enhancing water solubility, Cemadotin maintains strong anticancer activity while being more suitable for experimental and potential therapeutic applications.

Anticancer Activity
Cemadotin hydrochloride exhibits robust inhibition of cancer cell proliferation across a wide range of tumor models. It blocks mitosis by interfering with microtubule assembly and disassembly, preventing successful chromosome segregation. This disruption of the mitotic process induces apoptosis in rapidly dividing cancer cells. Reported Ki value is ~1 μM for tubulin inhibition, confirming strong potency at the molecular level.

Preclinical Applications

• Suppression of tumor xenograft growth in mouse models

• Inhibition of human cancer cell lines in vitro, including breast, lung, prostate, and hematological malignancies

• Mechanistic studies of tubulin-targeting anticancer agents

• Combination therapy studies with DNA-damaging agents, kinase inhibitors, or immunotherapies

Key Features

• Synthetic water-soluble analogue of Dolastatin 15

• Tubulin inhibitor with defined Ki value of 1 μM

• Induces mitotic arrest and apoptosis in tumor cells

• Effective in vitro and in vivo anticancer research models

• Suitable for mechanistic, pharmacological, and preclinical oncology studies

Product Specifications

Mechanism of Action

Cemadotin hydrochloride exerts its anticancer effects by inhibiting tubulin polymerization, a key process in mitotic spindle formation and cell cycle progression.

1. Tubulin Binding and Inhibition

   • Interferes with microtubule assembly and disassembly

   • Exhibits Ki ~1 μM for tubulin binding

   • Destabilizes mitotic spindles, preventing chromosome segregation

2. Mitotic Arrest

   • Cells treated with Cemadotin accumulate in the G2/M phase

   • Mitotic arrest triggers apoptotic pathways due to prolonged spindle checkpoint activation

3. Apoptotic Induction

   • Increases caspase activity and DNA fragmentation in cancer cells

   • Selectively induces apoptosis in proliferating tumor cells compared to normal cells

4. Preclinical Efficacy

   • Suppresses tumor xenograft growth in murine models

   • Enhances efficacy of combination treatments targeting DNA and signaling pathways

   • Provides a valuable model for studying microtubule-targeting anticancer drugs

     

Side Effects

In preclinical and experimental settings, the following effects have been observed:

• Cytotoxicity: Dose-dependent inhibition of cancer cell proliferation

• Apoptosis Induction: Strong activation of apoptotic signaling pathways

• Off-Target Toxicity: At higher concentrations, may affect non-tumor cells

• Animal Studies: Reported body weight loss and myelosuppression in murine models

Proper laboratory handling, dosing control, and protective measures are essential to minimize experimental toxicity.

Disclaimer

For laboratory research use only. Not for human use, medical diagnosis, or therapeutic application.

Keywords

Cemadotin hydrochloride, LU103793, CAS 172837-41-1, Dolastatin 15 analogue, tubulin inhibitor, mitotic arrest, apoptosis inducer, cancer research peptide, microtubule-targeting agent, anticancer drug development

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