[CAS NO. 917879-39-1] MK-2461
PRODUCTS SPECIFICATIONS [917879-39-1]
DESCRIPTION [917879-39-1]
Overview
| MDL | MFCD11977739 |
|---|---|
| Molecular Weight | 495.55 |
| Molecular Formula | C24H25N5O5S |
| SMILES | O=S(N(C)C[C@H]1OCCOC1)(NC2=CC=C3C=CC(C(C(C3=C2)=O)=C4)=NC=C4C5=CN(N=C5)C)=O |
1 Publications Citing Use of MCE
Summary
MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met with a mean IC50 of 2.5 nM. IC50 value: 2.5 nM [1] Target: c-Met in vitro: MK-2461 inhibits the kinase activity of human c-Met with a mean IC50 of 2.5 nM in the presence of 50 μM ATP. Ron (IC50 = 7 nM) and Flt1 (IC50 = 10 nM) are inhibited by MK-2461 with similar potencies to c-Met (IC50 = 2.5 nM), whereas nine other kinases, including FGFR1 , FGFR2 , FGFR3 , PDGFRβ , KDR, Flt3 , Flt4, TrkA , and TrkB , are found to be 8- to 30-fold less sensitive to MK-2461 than c-Met. [1] in vivo: MK-2461 inhibits c-Met signaling and tumor growth in tumor xenograft models in mice.[1]
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00518739 | Merck Sharp & Dohme LLC |
Advanced Cancer
|
February 2007 | Phase 1 |
| NCT00496353 | Merck Sharp & Dohme LLC |
Neoplasm
|
June 2007 | Phase 1|Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 31 mg/mL ( 62.56 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0180 mL | 10.0898 mL | 20.1796 mL |
| 5 mM | 0.4036 mL | 2.0180 mL | 4.0359 mL |
| 10 mM | 0.2018 mL | 1.0090 mL | 2.0180 mL |
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1.
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Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution