AMG-337 [1173699-31-4]
Katalog-Nummer HY-18696-1ml
Size : 10mM/1mL
Marke : MedChemExpress
AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC50 values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis.
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AMG-337 Chemische Struktur
CAS. Nr. : 1173699-31-4
This product is a controlled substance and not for sale in your territory.
Based on 1 publication(s) in Google Scholar
Beschreibung |
AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC50 values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis[1][2]. |
IC50 & Target |
IC50: 1 (WT MET), 1 (H1094R MET), 4.7 (M1250T MET), 5 (HGF-stimulated pMET (PC3 cells) MET), 21.5 (V1092I MET), 1077 (Y1230H MET) and >4000 nM (D1228H MET)[1] |
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In Vitro |
AMG 337 (0-3 µM; 72 h) inhibits proliferation in MET-dependent cancer cell lines[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis Analysis[1]
Cell Cycle Analysis[1]
Western Blot Analysis[1]
Western Blot Analysis[1]
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In Vivo |
AMG 337 (0-30 mg/kg; p.o.; daily, for 28 d) inhibits MET signaling in tumor xenografts and inhibits tumor growth in MET-dependent tumor xenograft models[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Klinische Studie |
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Molekulargewicht |
463.46 |
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Formel |
C23H22FN7O3 |
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CAS. Nr. |
1173699-31-4 |
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Appearance |
Solid |
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Color |
White to off-white |
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SMILES |
O=C1C2=C(N=CC(OCCOC)=C2)C=CN1[C@@H](C3=NN=C4C(F)=CC(C5=CN(C)N=C5)=CN43)C |
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Versand | Room temperature in continental US; may vary elsewhere. |
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Speicherung |
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Lösungsmittel & Löslichkeit |
In Vitro:
DMSO : 100 mg/mL (215.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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Reinheit & Dokumentation |
Purity: 99.43% |
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Verweise |
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Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.1577 mL | 10.7884 mL | 21.5768 mL | 53.9421 mL |
5 mM | 0.4315 mL | 2.1577 mL | 4.3154 mL | 10.7884 mL | |
10 mM | 0.2158 mL | 1.0788 mL | 2.1577 mL | 5.3942 mL | |
15 mM | 0.1438 mL | 0.7192 mL | 1.4385 mL | 3.5961 mL | |
20 mM | 0.1079 mL | 0.5394 mL | 1.0788 mL | 2.6971 mL | |
25 mM | 0.0863 mL | 0.4315 mL | 0.8631 mL | 2.1577 mL | |
30 mM | 0.0719 mL | 0.3596 mL | 0.7192 mL | 1.7981 mL | |
40 mM | 0.0539 mL | 0.2697 mL | 0.5394 mL | 1.3486 mL | |
50 mM | 0.0432 mL | 0.2158 mL | 0.4315 mL | 1.0788 mL | |
60 mM | 0.0360 mL | 0.1798 mL | 0.3596 mL | 0.8990 mL | |
80 mM | 0.0270 mL | 0.1349 mL | 0.2697 mL | 0.6743 mL | |
100 mM | 0.0216 mL | 0.1079 mL | 0.2158 mL | 0.5394 mL |