Fig. 1 · Structure

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MK-2461

Cat. No. A11753 CAS 917879-39-1

c-Met Inhibitor

MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.

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Biological Activity

Target & Activity

Target Activity Value
c-Met(M1250T) IC50 0.4nM
c-Met(Y1235D) IC50 0.5nM
c-Met(Y1230H) IC50 1.0nM
c-Met(N1100) IC50 1.5nM
c-Met(Y1230C) IC50 1.5nM
c-Met IC50 2.5nM
RON IC50 7nM
FLT1 IC50 10nM
FLT3 IC50 22nM
PDGFRβ IC50 22nM
Mer IC50 24nM
FGFR2 IC50 39nM
KDR IC50 44nM
TrkA IC50 46nM
FGFR3 IC50 50nM
TrkB IC50 61nM
FGFR1 IC50 65nM
FLT4 IC50 78nM
DRAK1 IC50 199nM
JAK2 IC50 225nM
IRAK4 IC50 298nM
MELK IC50 606nM
RET IC50 635nM
DYRK2 IC50 1.143μM
MLK1 IC50 4.303μM
IRAK1 IC50 5.459μM
Abl IC50 7.747μM

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Cellular Effect

Cell Line Activity Value Description Reference
GTL 16 cell line IC50 440 nM Antiproliferative activity against human GTL16 cells after 72 hrs [PMID: 21608528]

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 917879-39-1
Applications c-Met Inhibitor
Formula C24H25N5O5S
Molecular Weight 495.6
SMILES
CN1C=C(C=N1)C2=CN=C3C=CC4=C(C=C(C=C4)NS(=O)(=O)N(C)C[C@@H]5COCCO5)C(=O)C3=C2

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 95 mg/mL (191.7 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
14 mg/mL
Vehicle
1% DMSO+30% polyethylene glycol+1% Tween 80, pH 4

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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