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Chemical Structure| 1848959-10-3 Chemical Structure| 1848959-10-3

Structure of TAS4464
CAS No.: 1848959-10-3

Chemical Structure| 1848959-10-3

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TAS4464 selectively inhibits NAE relative to the other E1s UAE and SAE.

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Product Details of TAS4464

CAS No. :1848959-10-3
Formula : C21H23FN6O6S
M.W : 506.51
SMILES Code : O[C@@H]1[C@H](O)[C@@H](CNS(=O)(N)=O)O[C@]1(N2C=C(C#CC3=C(OCC)C=CC=C3F)C4=C(N)N=CN=C24)[H]
MDL No. :MFCD32067967
InChI Key :TZTRUHFXPVXWRD-QTQZEZTPSA-N
Pubchem ID :124121703

Safety of TAS4464

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319
Precautionary Statements:P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human BJ-5ta cells 2000 nM 72 hours To assess the antiviral activity of TAS4464 against HCMV Viruses. 2021 Aug 14;13(8):1610
MHCC97H cells 100 nM 12 hours Inhibit PCNA NEDDylation, reduce PCNA protein expression, thereby inhibiting HCC cell growth Cell Death Dis. 2025 Mar 31;16(1):228
HCCLM3 cells 100 nM 12 hours Inhibit PCNA NEDDylation, reduce PCNA protein expression, thereby inhibiting HCC cell growth Cell Death Dis. 2025 Mar 31;16(1):228
Human MRC-5 cells 100-2000 nM 24 hours To assess the stabilization of CRL substrate p21 by TAS4464 Viruses. 2021 Aug 14;13(8):1610
C57BL/6 immortalized mouse embryonic fibroblasts (CIM) 100-2000 nM 24 hours 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 Viruses. 2021 Aug 14;13(8):1610
BALB/c immortalized mouse embryonic fibroblasts (BIM) 100-2000 nM 72 hours 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

In Vivo:

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. Invest New Drugs. 2021 Aug;39(4):1036-1046
BALB/c nude mice Subcutaneous tumor model Intraperitoneal injection 50 mg/kg Once a week, for 45 days Inhibit PCNA NEDDylation, reduce PCNA protein expression, thereby inhibiting HCC cell growth Cell Death Dis. 2025 Mar 31;16(1):228
SCID mice Human-MM xenograft model Intravenous 50 or 100 mg/kg Twice a week for 3 weeks 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. Cancer Sci. 2019 Dec;110(12):3802-3810

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02978235 Multiple Myeloma|NonHodgkin Ly... More >>mphoma Less << PHASE1 TERMINATED 2018-02-01 Center for Cancer and Blood Di... More >>sorders, Bethesda, Maryland, 20817, United States|Dana-Farber Cancer Institute, Boston, Massachusetts, 02215, United States|Weisberg Cancer Treatment Center, Farmington Hills, Michigan, 48334, United States|Mayo Clinic, Rochester, Minnesota, 55905, United States|John Theurer Cancer Center at Hackensack Meridian Health, Hackensack, New Jersey, 07601, United States|Icahn School of Medicine at Mount Sinai, New York, New York, 10029, United States|Gabrail Cancer Center, Canton, Ohio, 44718, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.87mL

1.97mL

0.99mL

19.74mL

3.95mL

1.97mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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