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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Almonertinib hydrochloride (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 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.
| ln Vitro |
NSCLC may be treated with almonertinib (HS-10296), an oral inhibitor of the EGFR mutant T790M that has possible anti-tumor activity [2]. Almonertinib (HS-10296) has the ability to inhibit G719X, del19, L858R, and L861Q, among other EGFR-sensitive mutations[3].
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| References |
[1]. 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.
[2]. 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. [3]. 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 |
| Molecular Formula |
C₃₀H₃₆CLN₇O₂
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|---|---|
| Molecular Weight |
562.11
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| CAS # |
2134096-03-8
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| Related CAS # |
Almonertinib;1899921-05-1;Almonertinib mesylate;2134096-06-1
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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.[H]Cl
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| Synonyms |
Almonertinib HS-10296 HCl HS 10296 HS10296
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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 : ~83.33 mg/mL (~148.25 mM)
H2O : ~12.5 mg/mL (~22.24 mM) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7790 mL | 8.8951 mL | 17.7901 mL | |
| 5 mM | 0.3558 mL | 1.7790 mL | 3.5580 mL | |
| 10 mM | 0.1779 mL | 0.8895 mL | 1.7790 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.
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