HS-10296 free base · Synonyms: HS 10296 · HS10296

Almonertinib 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

HS-10296 structure

CAS No.: 1899921-05-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 450.00	BP-02147-250mg	In stock	Get quote
500 mg	USD 700.00	BP-02147-500mg	In stock	Get quote
1 g	USD 1,100.00	BP-02147-1g	In stock	Get quote
2 g	USD 1,650.00	BP-02147-2g	In stock	Get quote
3 g	USD 1,950.00	BP-02147-3g	In stock	Get quote
5 g	Inquire	BP-02147-5g	In stock	Inquire

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Description

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.

Biological activity

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.

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
InChIKey: DOEOECWDNSEFDN-UHFFFAOYSA-N

Specifications

MW (average): 525.6446
Formula: C₃₀H₃₅N₇O₂
CAS No.: 1899921-05-1
Physical state: Solid
Color: Off-white to light 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 -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

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;S1556-0864(20)30714-0.

[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.

[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.

Same target

Search EGFR

Same research area

Search Cancer