Tozasertib
VE465 · VX 680 · VE 465 · CS-176 · VE-465 · VX-860 · MK 0457 · Tozasertib
Identifikatoren & physikalische Daten
| CAS No. | 639089-54-6 |
|---|---|
| Summenformel | C23H28N8OS |
| Durchschnittliche Molmasse | 464,599 g/mol |
| Monoisotopische Masse | 464,21067852 g/mol |
| SMILES | Cc1cc(Nc2cc(N3CCN(C)CC3)nc(Sc3ccc(NC(=O)C4CC4)cc3)n2)n[nH]1 |
| InChIKey | GCIKSSRWRFVXBI-UHFFFAOYSA-N |
| PubChem CID | 5494449 |
| ChEMBL | CHEMBL572878 |
| ChEBI | CHEBI:91336 |
| DTXSID | DTXSID10213609 |
Chemische & physikalische Eigenschaften
| Schmelzpunkt | 248-253°C (dec.) |
|---|---|
| Dichte | 1.40±0.1 g/cm3(Predicted) |
| Lagerbedingungen | 2-8°C |
| Löslichkeit | Soluble in DMSO (up to 100 mg/ml). |
| Aggregatzustand | powder |
| pKa (Säurekonstante) | 14.09±0.70(Predicted) |
| Farbe | white to beige |
| Stabilität | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
Sicherheit & Vorschriften
| Alarmwort | Warnung |
|---|---|
| Gefahrenhinweise | Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code H302 |
Anwendungen & Verwendung
Beschreibung
The Aurora kinases (A, B, and C) are a family of serine-threonine kinases that regulate various stages of mitotic function. With significant roles in cell cycle and cell division, Aurora kinase gene amplification and overexpression are linked to tumorigenesis. MK-0457 is a potent pan-Aurora kinase inhibitor but favors Aurora A (Ki = 0.6 nM) over Aurora B (Ki = 18 nM) or Aurora C (Ki = 4.6 nM). It shows selectivity against a panel of more than 190 different protein kinases. MK-0457 effectively inhibits proliferation of several different cell lines of clear cell renal carcinoma (IC50s = 2/M phase.
Verwenden
Tozasertib is used as a multikinase inhibitor once used for cancer treatment.