TizatERKib 是一种选择性ERK2抑制剂，IC50为 0.6 nM。详细信息请参考专利文献 WO2017080979A1 中的化合物 example 18。

AZD-0364 is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1 (example 18; IC50: 0.6 nM).

AZD-0364 is measured in the ERK2 mass spectrometry and A375 phospho-p90RSK assays (IC50s: 0.6 nM and 5.7 nM). AZD-0364 can inhibit the growth of a panel of cancer cell lines (A549, H2122, H2009, and Calu6 cell lines) with KRAS mutations as monotherapy.

In the A549 xenograft model, Selumetinib is dosed twice daily (BiD) 8 hours apart and AZD-0364 ethanesulfonic acid is dosed once daily (QD) 4 hours after the first Selumetinib dose. Both compounds are dosed continuously for 3 weeks. Both vehicles are dosed in the vehicle group. Both Selumetinib and AZD-0364 ethanesulfonic acid reduce tumor growth relative to vehicle-only control. The combination of Selumetinib and AZD-0364 ethanesulfonic acid results in a reduction in tumor growth.

2097416-76-5

C24H24F2N8O2

494.5

AZD-0364

DMSO:100 mg/mL (202.22 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years