≥98% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
TAS4464 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 (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.
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.
Cell Research(from reference)
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
| Canonical Smiles | CCOC1=C(C(=CC=C1)F)C#CC2=CN(C3=NC=NC(=C23)N)C4C(C(C(O4)CNS(=O)(=O)N)O)O |
|---|---|
| IUPAC Name | 4-amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]oxolan-2-yl]-5-[2-(2-ethoxy-6-fluorophenyl)ethynyl]pyrrolo[2,3-d]pyrimidine |
| InChIKey | TZTRUHFXPVXWRD-QTQZEZTPSA-N |
| INCHI | 1S/C21H23FN6O6S/c1-2-33-14-5-3-4-13(22)12(14)7-6-11-9-28(20-16(11)19(23)25-10-26-20)21-18(30)17(29)15(34-21)8-27-35(24,31)32/h3-5,9-10,15,17-18,21,27,29-30H,2,8H2,1H3,(H2,23,25,26)(H2,24,31,32)/t15-,17-,18-,21-/m1/s1 |
| Isomeric SMILES | CCOC1=C(C(=CC=C1)F)C#CC2=CN(C3=NC=NC(=C23)N)[C@H]4[C@@H]([C@@H]([C@H](O4)CNS(=O)(=O)N)O)O |
| PubChem CID | 124121703 |
| Molecular Weight | 506.51 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Date | Item |
|---|---|---|---|
 L2320225 | Certificate of Analysis | Dec 09, 2023 | T414219 |
| L2320249 | Certificate of Analysis | Dec 09, 2023 | T414219 |
| L2320251 | Certificate of Analysis | Dec 09, 2023 | T414219 |
| L2320252 | Certificate of Analysis | Dec 09, 2023 | T414219 |
| L2320253 | Certificate of Analysis | Dec 09, 2023 | T414219 |
| Solubility | Solubility (25°C) In vitro DMSO: 100 mg/mL (197.42 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|---|
| Molecular Weight | 506.500 g/mol |
| XLogP3 | 0.200 |
| Hydrogen Bond Donor Count | 5 |
| Hydrogen Bond Acceptor Count | 12 |
| Rotatable Bond Count | 8 |
| Exact Mass | 506.138 Da |
| Monoisotopic Mass | 506.138 Da |
| Topological Polar Surface Area | 196.000 Ų |
| Heavy Atom Count | 35 |
| Formal Charge | 0 |
| Complexity | 911.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 4 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
