製品番号: HY-112823

Almonertinib

(別名: HS-10296)

9 Cited Publications

カスタマーレビュー

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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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: 99.83%
CAS 番号: 1899921-05-1
分子式: C₃₀H₃₅N₇O₂
分子量:525.64

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Almonertinib 構造式

CAS 番号: 1899921-05-1

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 臨床実験
化学情報
Publications (9)
溶剤 & 溶解度
- 体外
- 体内
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^[1]

EGFR^T790M

0.37 nM (IC₅₀)

EGFR^L858R/T790M

0.29 nM (IC₅₀)

EGFR^{del19 T790M}

0.21 nM (IC₅₀)

EGFR 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
A-431	IC₅₀	208.7 nM Compound: 6b-1	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	[PMID: 33667898]
A-431	IC₅₀	208.7 nM Compound: 35	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	[PMID: 38879996]
NCI-H1975	IC₅₀	1.44 nM Compound: 6b-1	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	[PMID: 33667898]
NCI-H1975	IC₅₀	1.44 nM Compound: 35	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	[PMID: 38879996]

体外実験

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.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1899921-05-1
性状 Solid
分子量 525.64
分子式 C₃₀H₃₅N₇O₂
Color Off-white to light yellow
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
別名

HS-10296
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	2 years
	-20°C	1 year

Publications (9)

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Journal Impact Factor

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.
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

IGF1R activates FOXP3-β-catenin signaling to promote breast cancer development. [Abstract]

2025 Jun;211(2):467-478. PMID: 40055251
Biochem Biophys Res Commun

2026 Feb 12:800:153165. PMID: 41548485
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
bioRxiv

2026 Mar 12.
Patent

US20220177473A1.

溶剤 & 溶解度

体外:

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)

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

1.9024 mL

9.5122 mL

19.0244 mL

5 mM

0.3805 mL

1.9024 mL

3.8049 mL

10 mM

0.1902 mL

0.9512 mL

1.9024 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, 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.

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)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 6.25 mg/mL (11.89 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 2% DMSO 40% PEG300 5% Tween-80 53% Saline

Solubility: 2 mg/mL (3.80 mM); Clear solution; Need ultrasonic

Working 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.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 5 mg/mL (9.51 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

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 (276 KB)
SDS (252 KB)
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- 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)
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]. 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]

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, 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

9 Cited Publications

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MedChemExpress（MCE）の使用を引用している文献 Almonertinib

EGFR 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 (9)

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

Almonertinib 関連分類

HY-112823 関連分類