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AMG-47a

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Catalog No. T7123Cas No. 882663-88-9

AMG-47a is a potent inhibitor of Lck and T cell proliferation. AMG-47a could promote the degradation of the KRAS oncoprotein. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.

AMG-47a

AMG-47a

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🥰Excellent
Purity: 98%
Catalog No. T7123Cas No. 882663-88-9
AMG-47a is a potent inhibitor of Lck and T cell proliferation. AMG-47a could promote the degradation of the KRAS oncoprotein. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$38In StockIn Stock
5 mg$89In StockIn Stock
10 mg$155In StockIn Stock
25 mg$262In StockIn Stock
50 mg$389In StockIn Stock
100 mg$573In StockIn Stock
1 mL x 10 mM (in DMSO)$97In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:98%
Appearance:Solid
Color:White
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Product Introduction

AMG-47a AI Summary
AMG-47a exhibits a variety of bioactivities and potent inhibitory effects on several kinases, including Lck, KDR, p38-alpha, Src, JNK1, JNK2, JNK3, Btk, and Yes1, with IC50 values in the nanomolar range. It also demonstrates notable inhibition of the NFkB signaling pathway (4726.9 nM) and exhibits cytotoxicity in a counterscreen for NFkB agonists and antagonists (20931.0 nM). Additionally, AMG-47a shows moderate potency in cell proliferation assays against the TMD8 cell line with caspase readouts at 8 and 16 hours (20931.0 nM and 2956.6 nM, respectively). It induces sensitization/mitigation effects in immunotoxin studies for HA22 and SS1P (6619.0 nM to 14818.0 nM) and demonstrates high potency in identifying gametocytocidal compounds (74266.1 nM). Furthermore, it inhibits T cell proliferation, IL2 secretion, and various cytokine productions in human and mouse models, and has moderate bioavailability, favorable protein binding properties, and pharmacokinetic parameters suitable for further development as a therapeutic agent targeting immune response pathways..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
AMG-47a is a potent inhibitor of Lck and T cell proliferation. AMG-47a could promote the degradation of the KRAS oncoprotein. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.
Targets&IC50
IL-2:21 nM (IC50), MLR:30 nM (IC50), JAK3:72 nM (IC50), VEGF2:1 nM (IC50), p38α:3 nM (IC50), Lck:0.2 nM (IC50)
Chemical Properties
Molecular Weight535.56
FormulaC29H28F3N5O2
Cas No.882663-88-9
SmilesCc1ccc(cc1-c1ccc2nc(NCCN3CCOCC3)ncc2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Relative Density.1.324 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 34 mg/mL (63.48 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8672 mL9.3360 mL18.6720 mL93.3602 mL
5 mM0.3734 mL1.8672 mL3.7344 mL18.6720 mL
10 mM0.1867 mL0.9336 mL1.8672 mL9.3360 mL
20 mM0.0934 mL0.4668 mL0.9336 mL4.6680 mL
50 mM0.0373 mL0.1867 mL0.3734 mL1.8672 mL

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TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

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All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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