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AMG410
🥰Excellent
Catalog No. T204083Cas No. 3040175-17-2
Alias AMG 410
AMG410 is a non-covalent, dual-modality KRAS inhibitor effective against both GDP (OFF) and GTP (ON) binding, with Kd (GDP) of 1 nM and Kd (GTP) of 22 nM, capable of blocking KRAS independently of the cell cycle. AMG410 does not affect HRAS and NRAS2, and exhibits high potency against KRAS G12D, G12V, G12C, G13D, and other mutants, with an IC₅₀ of 1–4 nM. It induces tumour regression and reduces phosphorylated ERK levels in KRAS-mutant cancer models.
AMG410
🥰Excellent
Purity: 99.84%
Catalog No. T204083Alias AMG 410Cas No. 3040175-17-2
AMG410 is a non-covalent, dual-modality KRAS inhibitor effective against both GDP (OFF) and GTP (ON) binding, with Kd (GDP) of 1 nM and Kd (GTP) of 22 nM, capable of blocking KRAS independently of the cell cycle. AMG410 does not affect HRAS and NRAS2, and exhibits high potency against KRAS G12D, G12V, G12C, G13D, and other mutants, with an IC₅₀ of 1–4 nM. It induces tumour regression and reduces phosphorylated ERK levels in KRAS-mutant cancer models.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $337 | In Stock | In Stock | |
| 5 mg | $693 | In Stock | In Stock | |
| 10 mg | $1,110 | In Stock | In Stock | |
| 25 mg | $1,890 | In Stock | In Stock | |
| 50 mg | $2,820 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:99.84%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | AMG410 is a non-covalent, dual-modality KRAS inhibitor effective against both GDP (OFF) and GTP (ON) binding, with Kd (GDP) of 1 nM and Kd (GTP) of 22 nM, capable of blocking KRAS independently of the cell cycle. AMG410 does not affect HRAS and NRAS2, and exhibits high potency against KRAS G12D, G12V, G12C, G13D, and other mutants, with an IC₅₀ of 1–4 nM. It induces tumour regression and reduces phosphorylated ERK levels in KRAS-mutant cancer models. |
| Targets&IC50 | KRas (G12D): 1-4 nM, KRas (G12V): 1-4 nM, KRAS (G13D): 1-4 nM |
| In vitro | Method: The inhibitory activity of AMG410 against various KRAS mutants was evaluated, along with its selectivity in different cell types and its binding affinity to KRAS-GTP and KRAS-GDP. Result: AMG410 exhibited potent inhibition of KRAS G12D, G12V, and G13D mutants (IC₅₀ = 1–4 nM), with a median IC₅₀ of 12 nM in KRAS-mutant tumor cells, and showed weak inhibition in non-transformed cells (IC₅₀ > 5 μM), indicating high selectivity. It bound both GTP- and GDP-bound KRAS (KD = 22 nM and 1 nM, respectively), enabling state-independent blockade of KRAS signaling.[1] |
| Synonyms | AMG 410 |
| Molecular Weight | 656.08 |
| Formula | C31H32ClF2N7O5 |
| Cas No. | 3040175-17-2 |
| Smiles | FC=1C=2C=3C4=C(C=C(Cl)C3CCCOC(=O)O[C@]5(CN(C=6C(C1N=C(OC[C@@]78N(C[C@H](F)C7)CCC8)N6)=CN2)CCOC5)[H])NN=C4 |
| Relative Density. | no data available |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||
| Solubility Information | DMSO: 4 mg/mL (6.1 mM), Sonication is recommended. | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
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 DMSO 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 DMSO stock solution to 400 μL PEG300 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 ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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