To assess the stabilization of CRL substrate p21 by TAS4464
Viruses. 2021 Aug 14;13(8):1610
MM.1S co-cultured with HS-5
0-1000 nM
48 hours
To evaluate the impact of the bone marrow microenvironment on the sensitivity to TAS4464, the effects of TAS4464 on MM.1S cells were not attenuated by co-culture with BMSC.
Cancer Sci. 2019 Dec;110(12):3802-3810
Primary mouse embryonic fibroblasts (MEF)
100-2000 nM
72 hours
To assess the antiviral activity of TAS4464 against MCMV
To assess the antiviral activity of TAS4464 against MCMV
Viruses. 2021 Aug 14;13(8):1610
OPM-2
149 nM
72 hours
To assess the growth inhibitory effect of TAS4464 in MM cells, TAS4464 inhibited proliferation of all cell lines, with the highest half‐maximal growth inhibitory concentration in OPM-2 cells.
Cancer Sci. 2019 Dec;110(12):3802-3810
MM.1S
3.62 nM
72 hours
To assess the growth inhibitory effect of TAS4464 in MM cells, TAS4464 inhibited proliferation of all cell lines, with the lowest half‐maximal growth inhibitory concentration in MM.1S cells.
Cancer Sci. 2019 Dec;110(12):3802-3810
TAS4464 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Human
Patients with advanced/metastatic solid tumors
Intravenous infusion
10-56 mg/m²
Weekly, every 28 days as a cycle
To evaluate the safety, tolerability, efficacy, pharmacokinetics, and pharmacodynamics of TAS4464. Results showed a dose-dependent effect on liver function, but no complete or partial responses were observed, with only one patient achieving prolonged stable disease.
To evaluate the antitumor activity of TAS4464 in vivo, TAS4464 significantly inhibited tumor growth and showed enhanced antitumor activity when combined with standard MM chemotherapies.
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