製品番号: HY-18303

AMG-47a

3 Cited Publications

カスタマーレビュー

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].

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.19%
CAS 番号: 882663-88-9
分子式: C₂₉H₂₈F₃N₅O₂
分子量:535.56

保管条件:

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

AMG-47a 構造式

CAS 番号: 882663-88-9

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

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Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (3)
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

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

Src アイソフォーム固有の製品をすべて表示 :

VEGFR アイソフォーム固有の製品をすべて表示 :

p38 MAPK アイソフォーム固有の製品をすべて表示 :

JAK アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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.

体内実験

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.

化学情報

CAS 番号 882663-88-9
性状 Solid
分子量 535.56
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (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)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

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MedChemExpress（MCE）の使用を引用している文献 AMG-47a

Src アイソフォーム固有の製品をすべて表示

VEGFR アイソフォーム固有の製品をすべて表示

p38 MAPK アイソフォーム固有の製品をすべて表示

JAK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (3)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

AMG-47a 関連分類

HY-18303 関連分類