hemiasterlin

Hemiasterlin is a cytotoxic peptide that acts by inducing mitotic arrest and abnormal spindle formation.

Hemiasterlin Derivative-1, a derivative of hemiasterlin, is utilized in the synthesis of Antibody-Drug Conjugates (ADC).

SPA107 (Hemiasterlin methyl ester) is an analogue of Hemiasterlin. It inhibits tubulin polymerization, exhibiting antimitotic activity with an IC50 of 0.5 nM. SPA107 also shows cytotoxicity against p53 mutated MCF-7 cells, with an IC50 of 0.5 nM.

Taltobulin trifluoroacetate is a synthetic analogue of the tripeptide hemiasterlin, is a potent agent of antimicrotubule that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.

Taltobulin hydrochloride is a synthetic analogue of the tripeptide hemiasterlin, is a potent agent of antimicrotubule that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.

E7974 is an analog of the sponge-derived anti-microtubule tripeptide hemiasterlin with antimitotic and potential antineoplastic activities. Hemiasterlin analog E7974 binds to the Vinca domain on tubulin, resulting in inhibition of tubulin polymerization and microtubule assembly; depolymerization of exsiting microtubules; inhibition of mitosis; and inhibition of cellular proliferation. This agent may have more affinity for the beta-3 tubulin isotype. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Taltobulin hydrochloride (HTI-286 hydrochloride), a synthetic analogue of the tripeptide hemiasterlin, effectively bypasses P-glycoprotein-mediated resistance both in vitro and in vivo as a robust antimicrotubule agent. It prevents the polymerization of purified tubulin, destabilizes cellular microtubule structures, and triggers both mitotic arrest and apoptosis [1].

SC239 is a 2-aminophenyl hemiasterlin-based agent-linker suitable for antibody-drug conjugate (ADC) applications. It features a tubulin-targeting warhead, SC209, connected through a cleavable valine-citrulline p-aminobenzyl carbamate linker equipped with dibenzocyclooctyne (DBCO). This drug-linker displays enhanced cytotoxic activity in Igrov1 cells with lower FolRα expression levels.