TAS4464

Catalog No.S8849 Batch:S884902

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Technical Data

Formula

C21H23FN6O6S

Molecular Weight 506.51 CAS No. 1848959-10-3
Solubility (25°C)* In vitro DMSO 100 mg/mL (197.42 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description TAS4464 is a potent and highly selective NEDD8 activating enzyme (NAE) inhibitor with IC50 of 0.955 nM. TAS4464 exhibits superior antitumor activity with prolonged target inhibition.
Targets
NAE [1]
(Cell-free assay)
0.955 nM
In vitro

TAS4464 selectively inhibits NAE relative to the other E1s UAE and SAE. TAS4464 treatment inhibits cullin neddylation and subsequently induces the accumulation of CRL substrates such as CDT1, p27, and phosphorylated IkBa in human cancer cell lines. Cytotoxicity profiling reveals that TAS4464 is highly potent with widespread antiproliferative activity not only for cancer cell lines, but also patient-derived tumor cells.[1]

In vivo

TAS4464 shows prolonged target inhibition in human tumor xenograft mouse models; weekly or twice a week TAS4464 administration led to prominent antitumor activity in multiple human tumor xenograft mouse models including both hematologic and solid tumors without marked weight loss.[1]

Protocol (from reference)

Cell Assay:

[1]

  • Cell lines

    PBMC, AML, DLBCL, SCLC cells. Patient-derived ovary and endometrial cells. Hepatocytes.

  • Concentrations

    1 nM, 10 nM, 100 nM, 1000 nM

  • Incubation Time

    24 h, 72 h, 6 days

  • Method

    PBMC, AML, DLBCL, and SCLC cells are treated with TAS4464 for 72 hours, after which viability is measured. Patient-derived ovary and endometrial cells are maintained in low-attachment plates and treated with TAS4464 or chemotherapeutic agents for 6 days. Cell viability is then measured by using the CellTiter-Glo 3D Cell Viability Assay. Hepatocytes are cultured in Cell-able plate for 10 days and then treated with TAS4464 for 24 hours, after which viability is measured by using CellTiter-Glo 3D Cell Viability Assay.

Animal Study:

[1]

  • Animal Models

    6-week-old female NOD-SCID mice

  • Dosages

    100 mg/kg, 75 mg/kg

  • Administration

    IV

Selleck's TAS4464 has been cited by 1 publication

The CUL5 E3 ligase complex negatively regulates central signaling pathways in CD8+ T cells [ Nat Commun, 2024, 15(1):603] PubMed: 38242867

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.