MK-2461

SKU: orb1223655

Description

MK-2461 is a potent multitargeted kinase inhibitor that preferentially inhibits c-Met with IC50 of 2.5 nM, with similar potencies for Ron and Flt1 (IC50=7 and 10 nM, respectively); 8- to 30-fold less sensitive to FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB; is equally or more potent against 5 c-Met mutants (N1100Y, Y1230C, Y1230H, Y1235D, and M1250T) with IC50 of 0.4-2.5 nM; inhibits c-Met-dependent mitogenesis, migration, cell scatter, and tubulogenesis in cells; suppresses tumor growth a murine xenograft model of c-Met-dependent gastric cancer; orally active.Solid Tumors Phase 2 Clinical

Key Properties

• CAS Number: 917879-39-1
• MW: 495.5508
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₅N₅O₅S
• SMILES: O=S(NC1=CC=C2C(C(C3=CC(C4=CN(C)N=C4)=CN=C3C=C2)=O)=C1)(N(C[C@H]5OCCOC5)C)=O
• Target: c-Met/HGFR
• Solubility: DMSO: ≥ 31 mg/mL

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 2461 | MK2461

Quick Database Links

Gene Symbol

c-Met/HGFR