VX-680 (MK-0457, Tozasertib)

Catalog No. A10981

VX-680 (MK-0457,Tozasertib)是一种有效的选择性Aurora激酶小分子抑制剂。
  • Sakamoto K, .et al. Recurrent 8q24 rearrangement in blastic plasmacytoid dendritic cell neoplasm: association with immunoblastoid cytomorphology, MYC expression, and drug response, Leukemia, 2018, May 23 PMID: 29795241
  • W. Joost Lesterhuis, .et al. Network analysis of immunotherapy-induced regressing tumours identifies novel synergistic drug combinations, Sci Rep, 2015, 5: 12298 PMID: 26193793
Catalog Num A10981
M. Wt 464.6
Formula C23H28N8OS
Purity >98%
Storage at -20°C 3 years Powder
CAS No. 639089-54-6
Synonyms
SMILES CC1=CC(=NN1)NC2=NC(=NC(=C2)N3CCN(CC3)C)SC4=CC=C(C=C4)NC(=O)C5CC5
VX-680 (MK-0457,Tozasertib)是一种有效的选择性Aurora激酶小分子抑制剂。
Targets
Aurora A (Cell-free assay) Aurora C (Cell-free assay) Aurora B (Cell-free assay) FLT3 (Cell-free assay) Bcr-Abl (Cell-free assay)
0.6 nM(Ki app)4.6 nM(Ki app)18 nM(Ki app)30 nM(Ki)30 nM(Ki)
In vitro (25°C) DMSO 90 mg/mL (193.71 mM)
Water Insoluble
Ethanol Insoluble
In vivo 5% DMSO+30% PEG 300+2% Tween 80+ddH2O 14 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq 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.
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 21.52 mL 107.62 mL 215.24 mL
0.5 mM 4.3 mL 21.52 mL 43.05 mL
1 mM 2.15 mL 10.76 mL 21.52 mL
5 mM 0.43 mL 2.15 mL 4.3 mL

*The above data is based on the productmolecular weight 464.6 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.