MK-5108

SKU: orb1227160

Description

MK-5108 (VX-689) is a potent, highly selective Aurora-A kinase inhibitor with IC50 of 0.064 nM, displays robust selectivity against Aurora-B (220-fold) and Aurora-C (190-fold) in the biochemical assays; also exhibits high selectivity for Aurora-A over a panel of 233 kinases, only one kinase (TrkA) with <100-fold selectivity; inhibits the growth of multiple human cancer cell lines in vitro and in human cancer xenograft models; MK-5108 significantly enhanced the efficacy of docetaxel without increasing its toxicity.Solid Tumors Phase 1 Clinical.

Key Properties

• CAS Number: 1010085-13-8
• MW: 461.94
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₁ClFN₃O₃S
• SMILES: OC(=O)[C@@]1(CC2=CC=CC(NC3=NC=CS3)=N2)CC[C@@H](CC1)OC1=C(F)C(Cl)=CC=C1 |r,c:7,13,16,26,30,32,t:5,11|
• Target: Aurora Kinase
• Solubility: DMSO: 6.4 mg/mL (Need Warming)

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MK 5108 | VX-689 | VX 689 | MK5108 | VX689

Quick Database Links

Gene Symbol

Aurora Kinase