MK-2461

Catalog No. A11753

MK-2461是一种新型的多靶点激酶抑制剂，优先抑制活化的c-Met受体。

Technical details

Catalog Num	A11753
M. Wt	495.6
Formula	C24H25N5O5S
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	917879-39-1
Synonyms	MK2461
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

Biological Activity

MK-2461是一种新型的多靶点激酶抑制剂，优先抑制活化的c-Met受体。

Targets

Target	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

Solubility *

In vitro (25°C)	DMSO	95 mg/mL (191.7 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	1% DMSO+30% polyethylene glycol+1% Tween 80, pH 4	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.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	20.18 mL	100.89 mL	201.78 mL
0.5 mM	4.04 mL	20.18 mL	40.36 mL
1 mM	2.02 mL	10.09 mL	20.18 mL
5 mM	0.4 mL	2.02 mL	4.04 mL

*The above data is based on the productmolecular weight 495.6 . 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.