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MedKoo Cat#: 575794 | Name: Almonertinib
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Almonertinib, also known as HS-10296 is an orally available inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity. Upon administration, HS-10296 binds to and inhibits EGFR T790M, a secondarily acquired resistance mutation, inhibits the tyrosine kinase activity of EGFR T790M, prevents EGFR T790M-mediated signaling and leads to cell death in EGFR T790M-expressing tumor cells. EGFR, a receptor tyrosine kinase that is mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.

Chemical Structure

Almonertinib
Almonertinib
CAS#1899921-05-1 (free base)

Theoretical Analysis

MedKoo Cat#: 575794

Name: Almonertinib

CAS#: 1899921-05-1 (free base)

Chemical Formula: C30H35N7O2

Exact Mass: 525.2852

Molecular Weight: 525.66

Elemental Analysis: C, 68.55; H, 6.71; N, 18.65; O, 6.09

Price and Availability

Size Price Availability Quantity
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,650.00 2 Weeks
1g USD 3,650.00 2 Weeks
2g USD 5,950.00 2 Weeks
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Related CAS #
1899921-05-1 (free base) 2134096-06-1 (mesylate) 2134096-03-8 (HCl) 2134096-04-9 (sulfate) 2134096-07-2 (fumarate) 2134096-08-3 (maleate)
Synonym
HS-10296; HS 10296; HS10296; Almonertinib; Ameile; Aumolertinib
IUPAC/Chemical Name
N-(5-((4-(1-cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide
InChi Key
DOEOECWDNSEFDN-UHFFFAOYSA-N
InChi Code
InChI=1S/C30H35N7O2/c1-6-29(38)32-24-17-25(28(39-5)18-27(24)36(4)16-15-35(2)3)34-30-31-14-13-23(33-30)22-19-37(20-11-12-20)26-10-8-7-9-21(22)26/h6-10,13-14,17-20H,1,11-12,15-16H2,2-5H3,(H,32,38)(H,31,33,34)
SMILES Code
C=CC(NC1=CC(NC2=NC=CC(C3=CN(C4CC4)C5=C3C=CC=C5)=N2)=C(OC)C=C1N(CCN(C)C)C)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
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).
In vitro activity:
HS-10296 significantly inhibited the proliferation of MDA-MB-231 cells with IC50 values at 24, 48 and 72 h of 8.393, 2.777 and 2.016 μmol/L, respectively. JC-1 and flow cytometry showed that HS-10296 induced obvious apoptosis of MDA-MB-231 cells, which showed an apoptosis rate of (21.63 ± 2.97)% following treatment with 8 μmol/L HS-10296. Reference: Nan Fang Yi Ke Da Xue Xue Bao. 2020 Jul 30;40(7):981-987. https://pubmed.ncbi.nlm.nih.gov/32895156/
In vivo activity:
Western blotting showed that compared with the control group, the expression levels of MMP-9, MMP-2 and vimentin protein in PC-9 and H1975 cells in 1, 2 and 4 µmol/L almonertinib treatment group were significantly lower, and the expression level of E-cadherin protein was significantly higher (all P<0.05). The experimental results of nude mice showed that compared with the control group and the positive control ositinib (AZD9291) group, the tumor growth was significantly inhibited, the weight of nude mice, the tumor volume and the tumor mass were significantly reduced in the almonertinib treatment group (all P<0.05). Reference: Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2021 Oct 28;46(10):1045-1053. https://pubmed.ncbi.nlm.nih.gov/34911833/
Solvent mg/mL mM
Solubility
DMSO 91.7 174.38
Ethanol 6.0 11.41
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 525.66 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Zhang Y, Zhang Y, Niu W, Ge X, Li X, Fan F, Li S, Liu H. Effect of almonertinib on the proliferation, invasion, and migration in non-small cell lung cancer cells. Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2021 Oct 28;46(10):1045-1053. English, Chinese. doi: 10.11817/j.issn.1672-7347.2021.201009. PMID: 34911833. 2. Ge X, Zhou Q, Zhang Y, Zhou W, Wu Y, Zhen C, Zhang M, Fan F, Chen G, Zhao J, Liu H. [EGFR tyrosine kinase inhibitor HS-10296 induces autophagy and apoptosis in triplenegative breast cancer MDA-MB-231 cells]. Nan Fang Yi Ke Da Xue Xue Bao. 2020 Jul 30;40(7):981-987. Chinese. doi: 10.12122/j.issn.1673-4254.2020.07.10. PMID: 32895156; PMCID: PMC7386211.
In vitro protocol:
1. Zhang Y, Zhang Y, Niu W, Ge X, Li X, Fan F, Li S, Liu H. Effect of almonertinib on the proliferation, invasion, and migration in non-small cell lung cancer cells. Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2021 Oct 28;46(10):1045-1053. English, Chinese. doi: 10.11817/j.issn.1672-7347.2021.201009. PMID: 34911833. 2. Ge X, Zhou Q, Zhang Y, Zhou W, Wu Y, Zhen C, Zhang M, Fan F, Chen G, Zhao J, Liu H. [EGFR tyrosine kinase inhibitor HS-10296 induces autophagy and apoptosis in triplenegative breast cancer MDA-MB-231 cells]. Nan Fang Yi Ke Da Xue Xue Bao. 2020 Jul 30;40(7):981-987. Chinese. doi: 10.12122/j.issn.1673-4254.2020.07.10. PMID: 32895156; PMCID: PMC7386211.
In vivo protocol:
1. Zhang Y, Zhang Y, Niu W, Ge X, Li X, Fan F, Li S, Liu H. Effect of almonertinib on the proliferation, invasion, and migration in non-small cell lung cancer cells. Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2021 Oct 28;46(10):1045-1053. English, Chinese. doi: 10.11817/j.issn.1672-7347.2021.201009. PMID: 34911833.
1: Zhang Y, Li Y, Han Y, Li M, Li X, Fan F, Liu H, Li S. Experimental study of EGFR-TKI aumolertinib combined with ionizing radiation in EGFR mutated NSCLC brain metastases tumor. Eur J Pharmacol. 2023 Feb 17:175571. doi: 10.1016/j.ejphar.2023.175571. Epub ahead of print. PMID: 36804545. 2: Zhang G, Tang X, Zhang X, Qiu X, Lai Q, Li J. Successful neoadjuvant treatment of EGFR exon 19 deletion combined with TP53 mutation in non-small cell lung cancer using aumolertinib after osimertinib-induced myocardial damage: a case report and literature review. Anticancer Drugs. 2023 Jan 4. doi: 10.1097/CAD.0000000000001496. Epub ahead of print. PMID: 36800249. 3: Hu Y, Quan YP, Duan YW, Li H, Shen J, Lin N, Wang C, Tian B, Li JJ. Aumolertinib effectively reduces clinical symptoms of an EGFR L858R-mutant non- small cell lung cancer case coupled with osimertinib-induced severe thrombocytopenia: a case report. Anticancer Drugs. 2023 Mar 1;34(3):455-459. doi: 10.1097/CAD.0000000000001424. Epub 2022 Oct 17. PMID: 36730569. 4: Tan S, Lu R, Yao D, Wang J, Gao P, Xie G, Liu H, Yao X. Identification of LRRK2 Inhibitors through Computational Drug Repurposing. ACS Chem Neurosci. 2023 Feb 1;14(3):481-493. doi: 10.1021/acschemneuro.2c00672. Epub 2023 Jan 17. PMID: 36649061. 5: Li J, Wang A, Li N, Zhu Y, Li K, Liu H, Gao Z. [Aumolertinib inhibits growth of human choroidal melanoma MUM-2B cells in vitro and in vivo]. Nan Fang Yi Ke Da Xue Xue Bao. 2022 Nov 20;42(11):1604-1610. Chinese. doi: 10.12122/j.issn.1673-4254.2022.11.03. PMID: 36504052; PMCID: PMC9742785. 6: Zhang Y, Zhang M, Cheng W, Fang S. Case report: Almonertinib in combination with bevacizumab for leptomeningeal metastases from epidermal growth factor receptor-mutation non-small cell lung cancer: Case series. Front Oncol. 2022 Nov 10;12:1040450. doi: 10.3389/fonc.2022.1040450. PMID: 36439478; PMCID: PMC9685536. 7: Zhang G, Yan B, Guo Y, Yang H, Li X, Li J. Case Report: A patient with the rare third-generation TKI-resistant mutation EGFR L718Q who responded to afatinib plus cetuximab combination therapy. Front Oncol. 2022 Oct 31;12:995624. doi: 10.3389/fonc.2022.995624. PMID: 36387265; PMCID: PMC9659857. 8: Chen W, Zhang L, Shen H, Wang B, Luo J, Cui E. Successful administration of low-dose almonertinib in a patient with lung adenocarcinoma after osimertinib- induced interstitial lung disease: a case report and literature review. Anticancer Drugs. 2023 Mar 1;34(3):460-466. doi: 10.1097/CAD.0000000000001436. Epub 2022 Nov 14. PMID: 36373747; PMCID: PMC9891277. 9: Zhang SS, Ou SI. Spotlight on Furmonertinib (Alflutinib, AST2818). The Swiss Army Knife (del19, L858R, T790M, Exon 20 Insertions, "uncommon-G719X, S768I, L861Q") Among the Third-Generation EGFR TKIs? Lung Cancer (Auckl). 2022 Oct 25;13:67-73. doi: 10.2147/LCTT.S385437. PMID: 36317157; PMCID: PMC9617553. 10: Ding X, Ding J, Leng Z, Song Y. Aumolertinib challenge as an optional treatment in advanced non small-cell lung cancer after osimertinib failure with epidermal growth factor receptor-sensitive mutation: A case series. Oncol Lett. 2022 Sep 22;24(5):400. doi: 10.3892/ol.2022.13520. PMID: 36276494; PMCID: PMC9533661. 11: Chen C, Zhang C, Lin H, Liu Q, Wu L, Zhou C, Zhang J. First-line therapeutic strategy for patients with advanced non-small cell lung cancer with Leu858Arg epidermal growth factor receptor mutations: a Bayesian network meta-analysis. Ther Adv Chronic Dis. 2022 Oct 17;13:20406223221125706. doi: 10.1177/20406223221125706. PMID: 36274751; PMCID: PMC9580106. 12: Fu Y, Li Y, Ma Y, He X, Xun X, Cui Y, Fan L, Dong Z. Effects of voriconazole and fluconazole on the pharmacokinetics of almonertinib in rats by UPLC-MS/MS. Biomed Chromatogr. 2023 Jan;37(1):e5525. doi: 10.1002/bmc.5525. Epub 2022 Oct 27. PMID: 36241418. 13: Lau SCM, Ou SI. And Still They Come Over Troubled Waters: Can Asia's Third- Generation EGFR Tyrosine Kinase Inhibitors (Furmonertinib, Aumolertinib, Rezivertinib, Limertinib, Befotertinib, SH-1028, and Lazertinib) Affect Global Treatment of EGFR+ NSCLC. J Thorac Oncol. 2022 Oct;17(10):1144-1154. doi: 10.1016/j.jtho.2022.08.016. PMID: 36192074. 14: Xu H, Yang G, Liu R, Yang Y, Li W, Li J, Hao X, Xing P, Wang Y. EGFR uncommon alterations in advanced non-small cell lung cancer and structural insights into sensitivity to diverse tyrosine kinase inhibitors. Front Pharmacol. 2022 Sep 16;13:976731. doi: 10.3389/fphar.2022.976731. PMID: 36188595; PMCID: PMC9523264. 15: Li L. Two non-small cell lung cancer (NSCLC) patients with brain metastasis harboring epidermal growth factor receptor (EGFR) G719X and L861Q mutations benefited from aumolertinib: two cases report and review of the literature. Heliyon. 2022 Aug 28;8(9):e10407. doi: 10.1016/j.heliyon.2022.e10407. PMID: 36119883; PMCID: PMC9474834. 16: Benjamin DJ, Nagasaka M. Freeing the Competition: Will Aumolertinib (AENEAS) Have a Fighting Chance Against Osimertinib (FLAURA)? J Clin Oncol. 2023 Feb 1;41(4):742-744. doi: 10.1200/JCO.22.01199. Epub 2022 Sep 12. PMID: 36095291. 17: Chen J, Wu X, Wang J. Double-dose icotinib may induce the emergence of the EGFR exon 20 T790M mutation in non-small cell lung cancer patients harboring EGFR-sensitive mutation. Front Oncol. 2022 Jul 26;12:898586. doi: 10.3389/fonc.2022.898586. PMID: 35957876; PMCID: PMC9362841. 18: Tang PF, Bao SS, Gao NY, Shao CF, Xie WF, Wu XM, Zhao LP, Xiao ZX. Development and Validation of a UHPLC-MS/MS Method for Quantitation of Almonertinib in Rat Plasma: Application to an in vivo Interaction Study Between Paxlovid and Almonertinib. Front Pharmacol. 2022 Jul 22;13:960311. doi: 10.3389/fphar.2022.960311. PMID: 35935882; PMCID: PMC9355496. 19: Ren KH, Qin WW, Wang Y, Peng JC, Hu WX. Detection of an EML4-ALK fusion mutation secondary to epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI) therapy for lung cancer: a case report. Ann Palliat Med. 2022 Jul;11(7):2503-2509. doi: 10.21037/apm-22-744. PMID: 35927783. 20: Li Y, Meng L, Ma Y, Li Y, Xing X, Guo C, Dong Z. Determination of Osimertinib, Aumolertinib, and Furmonertinib in Human Plasma for Therapeutic Drug Monitoring by UPLC-MS/MS. Molecules. 2022 Jul 13;27(14):4474. doi: 10.3390/molecules27144474. PMID: 35889345; PMCID: PMC9325192.