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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-YK-029A
YK-029A

Chemical Structure : YK-029A

CAS No.: 2064269-82-3

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YK-029A (Pruvonertinib, YK029A)

货号: PC-24172Not For Human Use, Lab Use Only.

Pruvonertinib (YK-029A) is potent, wild-type sparing and mutant-selective inhibitor of EGFR T790 M and exon 20 insertion mutations with IC50 of 0.37 nM (EGFR L858R/T790 M), 29-fold selective over EGFR wt.

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10 mg ￥4580 In stock
25 mg ￥7580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Pruvonertinib (YK-029A) is potent, wild-type sparing and mutant-selective inhibitor of EGFR T790 M and exon 20 insertion mutations with IC50 of 0.37 nM (EGFR L858R/T790 M), 29-fold selective over EGFR wt.
YK-029A exhibits superior ntiproliferation effects in PC-9 (EGFRdel19), HCC827 (EGFRdel19), H1975 (EGFRLR/TM), and Ba/F3 (EGFRex20ins) cell lines
YK-029A also shows potent antiproliferation effects in EGFRex20ins expressing Ba/F3 cells with relatively good wt-EGFR selectivity (4-78 fold) in contrast to osimertinib.
YK-029A reduces pEGFR levels in the presence of EGF stimulation in H1975 cells, with reduction of pAKT levels led to the concomitant reduction in the downstream pERK levels.
YK-029A is effective with oral administration in vivo.
YK-029A (80 mg/kg, oral) exhibited significant antitumor activity in EGFRex20ins-driven patients-derived xenograft (PDX) models, preventing tumor progression or causing tumor regression.

物理化学性质&存储条件

分子量 500.61
分子式 C27H32N8O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(8-methylimidazo[1,2-a]pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide

参考文献

1. Liu B, et al. Eur J Med Chem. 2023 Oct 5;258:115590.

2. Duan J, et al. J Thorac Oncol. 2024 Feb;19(2):314-324.

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