Art. -Nr.: HY-18303

AMG-47a

3 Cited Publications

Kundenbewertung

Based on 3 publication(s) in Google Scholar

AMG-47a is an orally active, ATP-competitive Lck inhibitor (IC₅₀=0.2 nM). AMG-47a inhibits VEGF2, p38α, p38α, Jak3, MLR, and IL-2 with IC₅₀ of 1 nM, 3 nM, 72 nM, 30 nM, and 21 nM, respectively. AMG-47a reduces T cell activation and the production of cytokines such as TGF-β, exerting anti-inflammatory and anti-fibrotic activities. AMG-47a can be used in the research of autoimmune diseases, pulmonary fibrosis, and KRAS mutation-associated cancers[1][2][3].

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Reinheit: 99.19%
CAS. Nr.: 882663-88-9
Formel: C₂₉H₂₈F₃N₅O₂
Molecular Weight:535.56

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AMG-47a Chemical Structure

CAS. Nr.: 882663-88-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 0.2 nM (Lck), 1 nM (VEGF2), 3 nM (p38α), 72 nM (Jak3), 30 nM (MLR), 21 nM (IL-2)^[2]

Alle Src Isoform-spezifische Produkte anzeigen :

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

Alle JAK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
T-cell	IC₅₀	21 nM Compound: 47	Inhibition of anti CD3/CD28-induced IL2 secretion in human T cells Inhibition of anti CD3/CD28-induced IL2 secretion in human T cells	[PMID: 16970394]
T-cell	IC₅₀	30 nM Compound: 47	Inhibition of human T cell proliferation by mixed lymphocyte reaction Inhibition of human T cell proliferation by mixed lymphocyte reaction	[PMID: 16970394]

In Vitro

AMG-47a (100 nM-5 μM; 48 h) significantly reduces the level of EGFP-KRAS^G12V protein in HeLa cells, without significant effect on EGFP protein^[1].
AMG-47a (0.2 nM; 5 min) effectively inhibits the phosphorylation of Lck in CD4⁺ T cells, wtih comparable function to that of Nintedanib (HY-50904)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AMG-47a (10-100 mg/kg; oral gavage; single dose) dose-dependently inhibits serum IL-2 levels in the mouse anti-CD3-induced inflammation model, with an ED₅₀ of 11 mg/kg, showing anti-inflammatory activity^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 882663-88-9
Appearance Solid
Molecular Weight 535.56
Formel C₂₉H₂₈F₃N₅O₂
Color Light yellow to yellow
SMILES

O=C(NC1=CC=CC(C(F)(F)F)=C1)C2=CC=C(C)C(C3=CC4=CN=C(NCCN5CCOCC5)N=C4C=C3)=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

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Journal Impact Factor

Cell Death Dis

The Lck inhibitor, AMG-47a, blocks necroptosis and implicates RIPK1 in signalling downstream of MLKL. [Abstract]

2022 Apr 1;13(4):291. PMID: 35365636
Oncogene

A modified gene trap approach for improved high-throughput cancer drug discovery. [Abstract]

2018 Aug;37(31):4226-4238. PMID: 29717260

AMG-47a purchased from MedChemExpress. Usage Cited in: Oncogene. 2018 Aug;37(31):4226-4238. [Abstract]

AMG-47 results in decreased ERK phosphorylation.
Arch Pharm (Weinheim)

Discovery of potent CSK inhibitors through integrated virtual screening and molecular dynamic simulation. [Abstract]

2024 Sep;357(9):e2400066. PMID: 38809025

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 34 mg/mL (63.48 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8672 mL

9.3360 mL

18.6720 mL

5 mM

0.3734 mL

1.8672 mL

3.7344 mL

10 mM

0.1867 mL

0.9336 mL

1.8672 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Carver J, et al. A high-throughput assay for small molecule destabilizers of the KRAS oncoprotein. PLoS One. 2014 Aug 5;9(8):e103836. [Content Brief]

[2]. DiMauro EF, et al. Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. J Med Chem. 2006 Sep 21;49(19):5671-86. [Content Brief]

[3]. Kagawa K, et al. The lymphocyte-specific protein tyrosine kinase-specific inhibitor A-770041 attenuates lung fibrosis via the suppression of TGF-β production in regulatory T-cells. PLoS One. 2022 Oct 27;17(10):e0275987. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8672 mL	9.3360 mL	18.6720 mL	46.6801 mL
	5 mM	0.3734 mL	1.8672 mL	3.7344 mL	9.3360 mL
	10 mM	0.1867 mL	0.9336 mL	1.8672 mL	4.6680 mL
	15 mM	0.1245 mL	0.6224 mL	1.2448 mL	3.1120 mL
	20 mM	0.0934 mL	0.4668 mL	0.9336 mL	2.3340 mL
	25 mM	0.0747 mL	0.3734 mL	0.7469 mL	1.8672 mL
	30 mM	0.0622 mL	0.3112 mL	0.6224 mL	1.5560 mL
	40 mM	0.0467 mL	0.2334 mL	0.4668 mL	1.1670 mL
	50 mM	0.0373 mL	0.1867 mL	0.3734 mL	0.9336 mL
	60 mM	0.0311 mL	0.1556 mL	0.3112 mL	0.7780 mL

AMG-47a

3 Cited Publications

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AMG-47a

Epigenetics Compound Library

Immunology/Inflammation Compound Library

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Publications Citing Use of MedChemExpress (MCE) AMG-47a

Alle Src Isoform-spezifische Produkte anzeigen

Alle VEGFR Isoform-spezifische Produkte anzeigen

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Alle JAK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG-47a Related Classifications

HY-18303 Related Classifications