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Purity: =99.44%
Almonertinib (HS10296) is a novel, potent, orally bioavailable, 3rd-generation irreversible inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity. HS-10296 attaches itself to the secondarily acquired resistance mutation EGFR T790M, inhibits the tyrosine kinase activity of EGFR T790M, stops EGFR T790M-mediated signaling, and causes tumor cells that express EGFR T790M to die. Tumor cell proliferation and tumor vascularization are significantly influenced by EGFR, a receptor tyrosine kinase that is mutated in a variety of tumor cell types.
| Targets |
EGFRT790M (IC50 = 0.37 nM); EGFRL858R/T790M (IC50 = 0.29 nM); EGFRdel19 T790M (IC50 = 0.21 nM)
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|---|---|
| ln Vitro |
HS-10296 is a potentially anti-tumor drug that is administered orally and inhibits the EGFR mutant form T790M, which may be used to treat non-small cell lung cancer[2]. Furthermore, HS-10296 may be able to suppress mutations that are sensitive to EGFR, such as G719X, del19, L858R, and L861Q[3].
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| ln Vivo |
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)[4].
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| Cell Assay |
NSCLC cells H1975 and PC-9 were cultured in vitro. The effects of almonertinib on the proliferation, apoptosis, invasion, and migration of H1975 and PC-9 cells were detected by CCK-8 assay, apoptotic assay and Transwell assay. The expression of invasion and migration related proteins was detected by Western blotting[4].
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| Animal Protocol |
Centrifuge H1975 cells, wash with PBS, and suspend in serum-free RPMI 1640 medium. Then inject 3 × 106 cells per mouse subcutaneously into the right shoulder of 4-6 week old nude mice. After the tumor grows to 100 mm3, it will be randomly divided into three groups, with 5 mice in each group. Each group will be given 0.2 mL of dimethyl sulfoxide, 5 mg/kg AZD9291, and 5 mg/kg of amitinib by gavage, once every two days. Monitor the weight and tumor size of nude mice before each injection. The tumor volume is 2/2 of its length and width, and the entire process lasts for 21 days[4].
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| References |
[4]. 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. doi: 10.11817/j.issn.1672-7347.2021.201009.
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| Additional Infomation |
Almonertinib is a third-generation EGFR tyrosine kinase inhibitor targeting EGFR-sensitizing and T790M resistance mutations. It is being investigated against advanced or metastatic EGFR-mutated non-small cell lung cancer (NSCLC).
Aumolertinib is an orally available inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity. Upon administration, aumolertinib 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. Drug Indication Treatment of lung cancer Mechanism of Action Almonertinib inhibits EGFR tyrosine kinase targeting EGFR-sensitizing and T790M resistance mutations. |
| Molecular Formula |
C30H35N7O2
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|---|---|
| Molecular Weight |
525.6446
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| Exact Mass |
525.285
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| Elemental Analysis |
C, 68.55 H, 6.71 N, 18.65 O, 6.09
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| CAS # |
1899921-05-1
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| Related CAS # |
Almonertinib mesylate;2134096-06-1;Almonertinib hydrochloride;2134096-03-8; 1899921-05-1; 2134096-04-9 (sulfate); 2134096-07-2 (fumarate); 2134096-08-3
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| PubChem CID |
121280087
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
39
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| Complexity |
823
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DOEOECWDNSEFDN-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
N-[5-[[4-(1-cyclopropylindol-3-yl)pyrimidin-2-yl]amino]-2-[2-(dimethylamino)ethyl-methylamino]-4-methoxyphenyl]prop-2-enamide
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| Synonyms |
Almonertinib; Ameile; HS-10296; HS 10296; HS10296; HS-10296; Aumolertinib; Ameile; HS-10297; Egfr T790M inhibitor HS-10296; Aumolertinib [USAN]; Aumolertinib
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~190.2 mM)
Ethanol: ~6 mg/mL (~11.4 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (11.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 6.25 mg/mL (11.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04687241 | Active Recruiting |
Drug: Placebo Almonertinib Drug: Almonertinib |
Non-small Cell Lung Cancer | Jiangsu Hansoh Pharmaceutical Co., Ltd. |
April 30, 2021 | Phase 3 |
| NCT05826483 | Recruiting | Drug: Almonertinib | Malignant Tumor of Lung Poor Performance Status |
Guangzhou Institute of Respiratory Disease |
January 1, 2022 | Phase 1 |
| NCT04841811 | Recruiting | Drug: Almonertinib | Lung Cancer | Guangdong Association of Clinical Trials |
June 20, 2022 | Phase 3 |
| NCT04882345 | Not yet recruiting | Drug: Almonertinib | EGFR Gene Mutation Lung Cancer |
Shanghai Chest Hospital | July 15, 2021 | Phase 2 |
| NCT04870190 | Not yet recruiting | Drug: Almonertinib Drug: Osimertinib |
NSCLC | Shanghai Chest Hospital | June 1, 2021 | Phase 3 |
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