Almonertinib mesylate salt form · mesylate · Parent HS-10296

Almonertinib mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor.

For research use only. Not for human or veterinary use.

Target EGFR

Research area Cancer

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Data Sheet SDS COA

Almonertinib mesylate structure

CAS No.: 2134096-06-1

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Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 480.00	BP-02147B-100mg	In stock	Get quote
250 mg	USD 950.00	BP-02147B-250mg	In stock	Get quote
500 mg	USD 1,500.00	BP-02147B-500mg	In stock	Get quote
1 g	USD 2,400.00	BP-02147B-1g	In stock	Get quote
2 g	USD 3,600.00	BP-02147B-2g	In stock	Get quote

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Description

Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate 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 mesylate is used for the research of the non-small cell lung cancer.

Biological activity

In Vitro HS-10296 mesylate 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 mesylate could also inhibit other EGFR sensitive mutations, including G719X, del19, L858R and L861Q.

Identifiers

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.CS(=O)(O)=O
InChIKey: WTEXJDGTVUQRQY-UHFFFAOYSA-N

Specifications

MW (average): 621.7500
Formula: C₃₁H₃₉N₇O₅S
CAS No.: 2134096-06-1
Physical state: Solid
Color: Light yellow to yellow
Shipping: 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: Powder 4°C, sealed storage, away from moisture; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO 31.25 mg/mL

Documents

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

[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.

Same target

Search EGFR

Same research area

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