Almonertinib
Based on 9 publication(s) in Google Scholar
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer.
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- Pureté: 99.83%
- CAS No.: 1899921-05-1
- Formule: C30H35N7O2
- Masse moléculaire:525.64
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
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Publications Citing Use of MedChemExpress (MCE) Almonertinib
More- Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
- Eur J Pharmacol. 2026 Jan 12:1011:178448. [Abstract]
- Front Pharmacol. 2021 May 14:12:671328. [Abstract]
- Transl Lung Cancer Res. 2025 Jun 30;14(6):2159-2179. [Abstract]
- Breast Cancer Res Treat. 2025 Jun;211(2):467-478. [Abstract]
- Biochem Biophys Res Commun. 2026 Feb 12:800:153165.
- Biol Methods Protoc. 2025 Feb 13;10(1):bpaf012. [Abstract]
- bioRxiv. 2026 Mar 12.
- Patent. US20220177473A1.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Flow Cytometry
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WB
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IF
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Cell Imaging/Staining
Voir tous les produits spécifiques à Isoform EGFR
More
Activité biologique
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EGFRT790M 0.37 nM (IC50) |
EGFRL858R/T790M 0.29 nM (IC50) |
EGFRdel19 T790M 0.21 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| A-431 | IC50 |
208.7 nM
Compound: 6b-1
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Cytotoxicity against human A-431 cells harboring wild-type EGFR measured after 72 hrs by celltiter-glo assay
Cytotoxicity against human A-431 cells harboring wild-type EGFR measured after 72 hrs by celltiter-glo assay
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[PMID: 33667898] |
| A-431 | IC50 |
208.7 nM
Compound: 35
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Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 38879996] |
| NCI-H1975 | IC50 |
1.44 nM
Compound: 6b-1
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Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant measured after 72 hrs by celltiter-glo assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant measured after 72 hrs by celltiter-glo assay
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[PMID: 33667898] |
| NCI-H1975 | IC50 |
1.44 nM
Compound: 35
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Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer glo assay
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer glo assay
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[PMID: 38879996] |
HS-10296 is an orally available inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity, which canbe used to treat NSCLC[2]. Additionaly, HS-10296 could also inhibit other EGFR sensitive mutations, including G719X, del19, L858R and L861Q[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1899921-05-1
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Appearance Solid
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Masse moléculaire 525.64
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Formule C30H35N7O2
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Color Off-white to light yellow
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SMILES
COC(C=C(N(C)CCN(C)C)C(NC(C=C)=O)=C1)=C1NC2=NC(C3=CN(C4CC4)C5=C3C=CC=C5)=CC=N2
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Synonyms
HS-10296
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]2023 Feb 21;4(2):100911. PMID: 36657446 -
Eur J Pharmacol
ROS-mediated senescence and autophagy inhibition drive 5-FU/Aumolertinib synergy in colorectal cancer. [Abstract]2026 Jan 12:1011:178448. PMID: 41352706 -
Front Pharmacol
Restricting Glutamine Uptake Enhances NSCLC Sensitivity to Third-Generation EGFR-TKI Almonertinib. [Abstract]2021 May 14:12:671328. PMID: 34054543
Almonertinib purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 May 14:12:671328. [Abstract]
CCK8 assay was used to detect different concentrations of Almonertinib (HS-10296) (2, 4, 8, and 16 µM) on H1975 and A549 cells for 24, 48, and 72 h.
Almonertinib purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 May 14:12:671328. [Abstract]
Flow cytometry was used to detect the apoptosis rate of different concentrations of Almonertinib (HS-10296) (4, 8,12 μM) on H1975 and A549 cells after 24 h.
Almonertinib purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 May 14:12:671328. [Abstract]
Western blotting (WB) was used to examine the expression of SLC1A5 protein in H1975 cells stimulated by Almonertinib (4, 8, 12 μM) at different times.
Almonertinib purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 May 14:12:671328. [Abstract]
Immunofluorescence was used to detect the expression of SLC1A5 protein in H1975 cells stimulated by Almonertinib (4, 8, 12 μM) at different times.
Almonertinib purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 May 14:12:671328. [Abstract]
Effects of Almonertinib (4, 8,12 μM) and V9302 alone or in combination on the colony forming ability.
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Transl Lung Cancer Res
Development of a 3D-3 co-culture microbead consisting of cancer-associated fibroblasts and human umbilical vein endothelial cells for the anti-tumor drug assessment of lung cancer. [Abstract]2025 Jun 30;14(6):2159-2179. PMID: 40673102 -
Breast Cancer Res Treat
2025 Jun;211(2):467-478. PMID: 40055251 -
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Biol Methods Protoc
Optimizing drug sensitivity assays in patient-derived tumor organoids: a comparison of IC50 estimation methods and experimental parameters. [Abstract]2025 Feb 13;10(1):bpaf012. PMID: 40060949 -
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Solvant et solubilité
DMSO : 80 mg/mL (152.20 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 6.25 mg/mL (11.89 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (9.51 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Yang JC, et al. Safety, Efficacy, and Pharmacokinetics of Almonertinib (HS-10296) in Pretreated Patients With EGFR-Mutated Advanced NSCLC: A Multicenter, Open-label, Phase 1 Trial [published online ahead of print, 2020 Sep 9]. J Thorac Oncol. 2020;S1556-0864(20)30714-0. [Content Brief]
[2]. Sullivan I, et al. Next-Generation EGFR Tyrosine Kinase Inhibitors for Treating EGFR-Mutant Lung Cancer beyond First Line. Front Med (Lausanne). 2017 Jan 18;3:76. [Content Brief]
[3]. Wu SG, et al. Management of acquired resistance to EGFR TKI-targeted therapy in advanced non-small cell lung cancer. Mol Cancer. 2018 Feb 19;17(1):38. [Content Brief]
Complete Stock Solution Preparation Table
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9024 mL | 9.5122 mL | 19.0244 mL | 47.5611 mL |
| 5 mM | 0.3805 mL | 1.9024 mL | 3.8049 mL | 9.5122 mL | |
| 10 mM | 0.1902 mL | 0.9512 mL | 1.9024 mL | 4.7561 mL | |
| 15 mM | 0.1268 mL | 0.6341 mL | 1.2683 mL | 3.1707 mL | |
| 20 mM | 0.0951 mL | 0.4756 mL | 0.9512 mL | 2.3781 mL | |
| 25 mM | 0.0761 mL | 0.3805 mL | 0.7610 mL | 1.9024 mL | |
| 30 mM | 0.0634 mL | 0.3171 mL | 0.6341 mL | 1.5854 mL | |
| 40 mM | 0.0476 mL | 0.2378 mL | 0.4756 mL | 1.1890 mL | |
| 50 mM | 0.0380 mL | 0.1902 mL | 0.3805 mL | 0.9512 mL | |
| 60 mM | 0.0317 mL | 0.1585 mL | 0.3171 mL | 0.7927 mL | |
| 80 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.5945 mL | |
| 100 mM | 0.0190 mL | 0.0951 mL | 0.1902 mL | 0.4756 mL |
Almonertinib Related Classifications
HY-112823 Related Classifications
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