Determine the necessary mass, volume, or concentration for preparing a solution.
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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≥99% ベースライン干渉を最小限に抑える必要がある、感度の高いクロマトグラフィーおよび分析ワークフロー向け。
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クロマトグラフィー、有機合成、クロスカップリング反応に関する 0 件の査読済み論文で引用されています。
Information
PRT-060318 2HCl PRT-060318 (PRT318) is a novel selective inhibitor of the Syk tyrosine kinase with an IC50 of 4 nM, as an approach to HIT treatment.
Targets
Syk (Cell-free assay) 4nM
In vitro
PRT318 inhibits platelet activation via GPVI/FcRγ, an ITAM receptor complex, but not via ADP or thrombin, which are G-protein coupled receptors. PRT318 effectively antagonizes CLL(chronic lymphocytic leukemia) cell survival after BCR triggering and in nurse-like cell-co-cultures. PRT318 inhibits Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering.
In vivo
In both rabbit and pig models, intravenous infusion of PRT060318 targets maximal inhibition of Syk kinase activity and significantly inhibits arterial thrombosis. The antithrombotic activity of PRT060318 in pigs is remarkable because it was achieved with complete inhibition of CVXN-induced platelet aggregation, with no effect on ADP-induced platelet aggregation, and no prolongation of ear bleeding time. Also, Syk inhibitor PRT318 is an active agent in HIT. Inhibition of Syk signaling with the orally bio-available PRT318 limits the thrombocytopenic and thrombotic effects of HIT IC in vivo.
Cell Research(from reference)
Cell lines:LY3,LY4,LY7,LY18 cell lines
Concentrations:0-3μM
Incubation Time:0-72h
危険性、取扱い、保管、および規制遵守を網羅した包括的な文書。
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| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| 分類 | Diazines |
| Subclass | Pyrimidines and pyrimidine derivatives |
| Intermediate Tree Nodes | Pyrimidinecarboxylic acids and derivatives |
| Direct Parent | Pyrimidinecarboxamides |
| Alternative Parents | Aniline and substituted anilines Toluenes Secondary alkylarylamines Aminopyrimidines and derivatives Cyclohexylamines Imidolactams Vinylogous amides Heteroaromatic compounds Amino acids and derivatives Primary carboxylic acid amides Azacyclic compounds Organic oxides Organooxygen compounds Organopnictogen compounds Hydrocarbon derivatives Monoalkylamines |
| Molecular Framework | Aromatic heteromonocyclic compounds |
| Substituents | Pyrimidinecarboxamide - Aniline or substituted anilines - Aminopyrimidine - Cyclohexylamine - Secondary aliphatic/aromatic amine - Toluene - Imidolactam - Benzenoid - Monocyclic benzene moiety - Heteroaromatic compound - Vinylogous amide - Carboxamide group - Primary carboxylic acid amide - Amino acid or derivatives - Azacycle - Secondary amine - Carboxylic acid derivative - Organopnictogen compound - Organooxygen compound - Organonitrogen compound - Primary aliphatic amine - Primary amine - Organic nitrogen compound - Amine - Organic oxygen compound - Hydrocarbon derivative - Organic oxide - Aromatic heteromonocyclic compound |
| 説明 | This compound belongs to the class of organic compounds known as pyrimidinecarboxamides. These are compounds containing a pyrimidine ring which bears a carboxamide. |
| External Descriptors | Not available |
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Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | 日付 | 商品 |
|---|---|---|---|
| Certificate of Analysis | Jan 14, 2023 | P413822 | |
| Certificate of Analysis | Jan 14, 2023 | P413822 | |
| Certificate of Analysis | Jan 14, 2023 | P413822 | |
| Certificate of Analysis | Jan 14, 2023 | P413822 | |
| Certificate of Analysis | Jan 14, 2023 | P413822 | |
| Certificate of Analysis | Jan 14, 2023 | P413822 | |
| Certificate of Analysis | Jan 14, 2023 | P413822 | |
| Certificate of Analysis | Jan 14, 2023 | P413822 | |
| Certificate of Analysis | Jan 14, 2023 | P413822 | |
| Certificate of Analysis | Jan 14, 2023 | P413822 | |
| Certificate of Analysis | Jan 14, 2023 | P413822 |
| 溶解度 | Solubility (25°C) In vitro DMSO: 75 mg/mL (181.44 mM); Water: 75 mg/mL (181.44 mM); Ethanol: Insoluble; |
|---|---|
| 分子量 | 340.400 g/mol |
| XLogP3 | 2.600 |
| Hydrogen Bond Donor Count | 4 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 5 |
| Exact Mass | 340.201 Da |
| Monoisotopic Mass | 340.201 Da |
| Topological Polar Surface Area | 119.000 Ų |
| Heavy Atom Count | 25 |
| Formal Charge | 0 |
| Complexity | 447.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 2 |
| 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 |