≥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
TAS0728 TAS0728 (TPC 107) is a potent, selective, orally active, irreversible and covalent-binding inhibitor of HER2 (human epidermal growth factor receptor 2) with IC50 of 13 nM. TAS0728 inihibits BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2 with IC50 of 4.9 nM, 8.5 nM, 31 nM, 65 nM, 33 nM, 25 nM, 86 nM and 36 nM, respectively. TAS0728 shows antitumor activity.
Targets
HER2 (Cell-free assay) 13 nM
In vitro
TAS0728 covalently binds to HER2 at C805 and selectively inhibits its kinase activity. Once TAS0728 binds to HER2 kinase, the inhibitory activity is not affected by a high ATP concentration. TAS0728 possesses high specificity for HER2 over wild-type EGFR. TAS0728 potently inhibits the phosphorylation of mutated HER2 and wild-type HER2. TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2, HER3, and downstream effectors, thereby inducing apoptosis of HER2-amplified breast cancer cells.
In vivo
TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2, HER3, and downstream effectors, thereby inducing apoptosis in tumor tissues of a xenograft model. TAS0728 induces tumor regression in mouse xenograft models bearing HER2 signal–dependent tumors and exhibits a survival benefit without any evident toxicity in a peritoneal dissemination mouse model bearing HER2-driven cancer cells.
Cell Research(from reference)
Cell lines：SK-BR-3 cells, A-431, AU565, BT-474, Calu-3, NCI-N87 cells, etc.
Concentrations：40 nM, 10-1000 nM
Incubation Time：3 h, 48 h, 72 h
| Pubchem Sid | 528767350 |
|---|---|
| Kanonisches Lächeln | CC1=C(C=CC(=C1C)NC(=O)C2=NN(C3=NC=NC(=C23)N)C4CCCN(C4)C(=O)C=C)CC(=O)N(C)C |
| IUPAC Name | 4-amino-N-[4-[2-(dimethylamino)-2-oxoethyl]-2,3-dimethylphenyl]-1-[(3R)-1-prop-2-enoylpiperidin-3-yl]pyrazolo[3,4-d]pyrimidine-3-carboxamide |
| InChIKey | JCCIICHPRAAMGK-GOSISDBHSA-N |
| INCHI | 1S/C26H32N8O3/c1-6-20(35)33-11-7-8-18(13-33)34-25-22(24(27)28-14-29-25)23(31-34)26(37)30-19-10-9-17(15(2)16(19)3)12-21(36)32(4)5/h6,9-10,14,18H,1,7-8,11-13H2,2-5H3,(H,30,37)(H2,27,28,29)/t18-/m1/s1 |
| PubChem CID | 130275856 |
| Molekulargewicht | 504.58 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →Full quality attributes and acceptance criteria for this grade.
View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Benzenoids |
| Klasse | Benzene and substituted derivatives |
| Subclass | Anilides |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Aromatic anilides |
| Alternative Parents | Phenylacetamides Pyrazolopyrimidines N-acylpiperidines Pyrimidines and pyrimidine derivatives N-acyl amines Imidolactams Tertiary carboxylic acid amides Pyrazolines Pyrazoles Heteroaromatic compounds Amino acids and derivatives Propargyl-type 1,3-dipolar organic compounds Azacyclic compounds Amidines Organopnictogen compounds Organooxygen compounds Organic oxides Monoalkylamines Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Aromatic anilide - Phenylacetamide - Pyrazolopyrimidine - N-acyl-piperidine - Fatty acyl - Imidolactam - Pyrimidine - Piperidine - N-acyl-amine - Fatty amide - Heteroaromatic compound - Tertiary carboxylic acid amide - Pyrazoline - Pyrazole - Azole - Carboxamide group - Amino acid or derivatives - Azacycle - Organoheterocyclic compound - Organic 1,3-dipolar compound - Propargyl-type 1,3-dipolar organic compound - Carboxylic acid derivative - Amidine - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Primary amine - Organooxygen compound - Organonitrogen compound - Primary aliphatic amine - Amine - Aromatic heteropolycyclic compound |
| Beschreibung | This compound belongs to the class of organic compounds known as aromatic anilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with an aromatic group. They have the general structure RNC(=O)R', where R= benzene, and R = aryl group. |
| External Descriptors | Not available |
Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Datum | Artikel |
|---|---|---|---|
 B2402098 | Certificate of Analysis | Jan 02, 2024 | T414209 |
| B2402099 | Certificate of Analysis | Jan 02, 2024 | T414209 |
| B2402100 | Certificate of Analysis | Jan 02, 2024 | T414209 |
| B2402147 | Certificate of Analysis | Jan 02, 2024 | T414209 |
| B2402150 | Certificate of Analysis | Jan 02, 2024 | T414209 |
| B2402156 | Certificate of Analysis | Jan 02, 2024 | T414209 |
| B2402157 | Certificate of Analysis | Jan 02, 2024 | T414209 |
| B2402163 | Certificate of Analysis | Jan 02, 2024 | T414209 |
| Löslichkeit | Solubility (25°C) In vitro DMSO: 100 mg/mL (198.18 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|---|
| Molekulargewicht | 504.600 g/mol |
| XLogP3 | 1.700 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 6 |
| Exact Mass | 504.26 Da |
| Monoisotopic Mass | 504.26 Da |
| Topological Polar Surface Area | 139.000 Ų |
| Heavy Atom Count | 37 |
| Formal Charge | 0 |
| Complexity | 869.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 1 |
| 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 |
