Almonertinib (Synonyms: HS-10296)

Name: Almonertinib
Brand: MedChemExpress
SKU: HY-112823
Rating: 5.0 (3 reviews)

Cat. No.: HY-112823 Purity: 99.98%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

Almonertinib Chemical Structure

CAS No. : 1899921-05-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 318	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 318	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 440	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 825	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1155	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1595	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Almonertinib:

3 Publications Citing Use of MCE Almonertinib

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View All Isoforms

EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

EGFR^T790M

0.37 nM (IC₅₀)

EGFR^L858R/T790M

0.29 nM (IC₅₀)

EGFR^{del19 T790M}

0.21 nM (IC₅₀)

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]
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]

In Vitro

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.

Clinical Trial

Molecular Weight

525.64

Formula

C₃₀H₃₅N₇O₂

CAS No.

1899921-05-1

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 83.33 mg/mL (158.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (250 KB) LCMS (265 KB)

Handling Instructions (2659 KB)

References

[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;S1556-0 [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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Almonertinib (Synonyms: HS-10296)

Customer Review

Other Forms of Almonertinib:

Almonertinib Related Antibodies

3 Publications Citing Use of MCE Almonertinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Almonertinib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Almonertinib Related Classifications

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Your Recently Viewed Products:

Customer Review

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