产品说明书

Zipalertinib

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Chemical Structure| 1661854-97-2 同义名 : TAS6417;CLN-081
CAS号 : 1661854-97-2
货号 : A1166647
分子式 : C23H20N6O
纯度 : 97%
分子量 : 396.445
MDL号 : MFCD31715430
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 20 mg/mL(50.45 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • EGFR/ErbB1

    EGFR WT, IC50:8 nM

    EGFR (L861Q), IC50:4.1 nM

  • ErbB4

    HER4, IC50:4 nM

  • mutant EGFR

    EGFR L858R, IC50:2 nM

    EGFR(d746-750), IC50:1.4 nM
描述 Zipalertinib is a potent, orally active and pan-mutagen-selective EGFR tyrosine kinase inhibitor with a unique scaffold that matches the ATP binding site of the EGFR hinge region and an IC50 value of 1.1-8.0 nM[1][2].Zipalertinib, also known as TAS6417, inhibits EGFR phosphorylation and downstream molecules in NSCLC cell lines expressing EGFR exon 20 insertions, leading to caspase activation[1].Zipalertinib exhibits potent inhibition of the most common EGFR mutations (exon 19 deletions and L858R), with the strongest inhibitory effect on cells harbouring EGFR-T790M, a 1st/2nd generation TKI resistance mutation. At concentrations of less than 10 μM, Zipalertinib inhibits cell proliferation and EGFR signalling in NSCLC cell lines carrying or not carrying the common T790M EGFR mutation[2].Zipalertinib covalently modifies the recombinant EGFR exon 20 in-frame insertion mutation at residue 797 cysteine to inhibit EGFR signalling, thereby inhibiting growth and inducing apoptosis in NSCLC cells driven by the EGFR exon 20 insertion mutation[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.61mL

2.52mL

1.26mL

25.22mL

5.04mL

2.52mL
参考文献

[1]Hasako S, et al. TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations. Mol Cancer Ther. 2018 Aug;17(8):1648-1658.

[2]Hibiki Udagawa, et al. TAS6417/CLN-081 Is a Pan-Mutation-Selective EGFR Tyrosine Kinase Inhibitor with a Broad Spectrum of Preclinical Activity against Clinically Relevant EGFR Mutations. Mol Cancer Res. 2019 Nov;17(11):2233-2243.