产品详情

生物活性

AMG-458是一种有效的c-Met抑制剂，IC50值为60nM，对VEGFR2具有选择性。

Targets

Target	Value
c-Met(H1094R)	ki: 0.5nM
c-Met(V1092I)	ki: 1.1nM
c-Met(Human)	ki: 1.2nM
c-Met(Mouse)	ki: 2.0nM
c-Met(D1228H)	ki: 2.2nM
c-Met(M1250T)	ki: 4.1nM
c-Met(Y1230H)	ki: 4.5nM
VEGFR2	ki: 4.1μM

溶解度 *

In vitro (25°C)	DMSO	18 mg/mL (33.35 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	15% Captisol+citrate vehicle	28 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.

制备储备液

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	18.53 mL	92.66 mL	185.32 mL
0.5 mM	3.71 mL	18.53 mL	37.06 mL
1 mM	1.85 mL	9.27 mL	18.53 mL
5 mM	0.37 mL	1.85 mL	3.71 mL

*The above data is based on the productmolecular weight 539.6 . 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.

化学数据

目录号	A11055
作用机制	Inhibitor (抑制剂)
M. Wt	539.6
Formula	C30H29N5O5
Purity	>99%
Storage	Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
CAS No.	913376-83-7
Synonyms	AMG458, AMG 458
SMILES	CC1=C(C(=O)N(N1CC(C)(C)O)C2=CC=CC=C2)C(=O)NC3=NC=C(C=C3)OC4=C5C=CC(=CC5=NC=C4)OC