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Almonertinib

Name: Almonertinib
Brand: TargetMol
SKU: T5462
Price: 91 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5462Cas No. 1899921-05-1

Alias HS-10296

Almonertinib (HS-10296) is an inhibitor specifically targeting EGFR activation mutations and the resistant EGFR T790M mutation, exhibiting limited activity against wild-type EGFR.

Almonertinib

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Purity: 99.99%

Catalog No. T5462Alias HS-10296Cas No. 1899921-05-1

Almonertinib (HS-10296) is an inhibitor specifically targeting EGFR activation mutations and the resistant EGFR T790M mutation, exhibiting limited activity against wild-type EGFR.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$91	In Stock	In Stock
5 mg	$207	In Stock	In Stock
10 mg	$328	In Stock	In Stock
25 mg	$553	In Stock	In Stock
50 mg	$796	In Stock	In Stock
100 mg	$1,090	In Stock	In Stock
500 mg	$2,220	-	In Stock
1 mL x 10 mM (in DMSO)	$262	In Stock	In 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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Batch Information

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Purity:99.99%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

Almonertinib AI Summary

Almonertinib exhibits potent antitumor activity against human NCI-H1975 cells harboring the EGFR L858R/T790M double mutant, resulting in an 83% tumor growth inhibition at a dosage of 5 mg/kg. It strongly inhibits recombinant human N-terminal GST-tagged EGFR T790M/L858R double mutant with an IC50 value of 0.18 nM and demonstrates a selectivity ratio of 16.1 compared to wild-type EGFR. Additionally, the compound shows significant antiproliferative activity in the mutant cells, with an IC50 value of 1.44 nM, while its cytotoxicity against human A-431 cells with wild-type EGFR is moderate, having an IC50 of 208.7 nM. This results in a selectivity ratio of 145.0 between the two cell types. Favorable pharmacokinetic properties in rats include a Tmax of 1.0 hr, a Cmax of 1004.45 nM, a half-life of 7.0 hr, and an oral bioavailability of 52.0%..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Almonertinib (HS-10296) is an inhibitor specifically targeting EGFR activation mutations and the resistant EGFR T790M mutation, exhibiting limited activity against wild-type EGFR.
Targets&IC50	EGFR (T790M):0.37 nM (IC50), EGFR (del19/T790M):0.21 nM (IC50), EGFR (L858R/T790M):0.29 nM (IC50)
Synonyms	HS-10296

Chemical Properties

Molecular Weight	525.64
Formula	C₃₀H₃₅N₇O₂
Cas No.	1899921-05-1
Smiles	COc1cc(N(C)CCN(C)C)c(NC(=O)C=C)cc1Nc1nccc(n1)-c1cn(C2CC2)c2ccccc12
Relative Density.	1.24 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 54.55 mg/mL (103.78 mM), Sonication is recommended.

Ethanol: 6 mg/mL (11.41 mM), Sonication is recommended.

H2O: Insoluble

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.51 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9024 mL	9.5122 mL	19.0244 mL	95.1221 mL
5 mM	0.3805 mL	1.9024 mL	3.8049 mL	19.0244 mL
10 mM	0.1902 mL	0.9512 mL	1.9024 mL	9.5122 mL

DMSO

	1mg	5mg	10mg	50mg
20 mM	0.0951 mL	0.4756 mL	0.9512 mL	4.7561 mL
50 mM	0.0380 mL	0.1902 mL	0.3805 mL	1.9024 mL
100 mM	0.0190 mL	0.0951 mL	0.1902 mL	0.9512 mL

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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, 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 DMSO TargetMol | 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 DMSO TargetMol | reagent 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 TargetMol | reagent 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.

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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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