AMG-458

This product is for research use only, not for human use. We do not sell to patients.

AMG-458
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Size Price Stock
250mg$1290Check With Us
500mg$2050Check With Us
1g$3075Check With Us

Cat #: V0600 CAS #: 913376-83-7 Purity ≥ 98%

Description: AMG 458 (AMG-458) is a novel c-Met inhibitor with potential anticancer activity.

References: Albrecht BK, et al. Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase. J Med Chem. 2008, 51(10), 2879-2882.

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Molecular Weight (MW)539.58
Molecular FormulaC30H29N5O5
CAS No.913376-83-7
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 21 mg/mL (38.9 mM)r
Water: <1 mg/mLr
Ethanol: <1 mg/mL
Solubility In Vivo15% Captisol+citrate vehicle: 30 mg/mL
SMILES CodeO=C(C1=C(C)N(CC(C)(O)C)N(C2=CC=CC=C2)C1=O)NC3=NC=C(OC4=CC=NC5=CC(OC)=CC=C45)C=C3
SynonymsAMG-458; AMG 458; AMG458;
ProtocolIn VitroAMG-208 (compound 4) treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM.
In VivoIn male Sprague Dawley rats, AMG-208 (0.5 mg/kg i.v.) shows a high bioavailability with Cl of 0.37 L/h/kg, Vss of 0.38 L/kg and T1/2 of 1 hour.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.8533 mL9.2665 mL18.5329 mL37.0659 mL
5mM0.3707 mL1.8533 mL3.7066 mL7.4132 mL
10mM0.1853 mL0.9266 mL1.8533 mL3.7066 mL
20mM0.0927 mL0.4633 mL0.9266 mL1.8533 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.