AMG-232 is a highly potent, selective and orally bioavailable piperidinone inhibitor of the MDM2-p53 interaction ((SPR KD= 0.045 nM, SJSA-1 EdU IC50=9.1 nM).
Navtemadlin 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HCT116 p53+/+
0.5 µM
24 hours
Evaluate the effect of Navtemadlin on HCT116 p53+/+ cells under hypoxia, results showed Navtemadlin significantly reduced the S phase cell population.
Sci Rep. 2023 Mar 20;13(1):4583.
B16-F10 p53+/+
2 µM
24 hours
Evaluate the effect of Navtemadlin on B16-F10 p53+/+ cells under hypoxia, results showed Navtemadlin significantly reduced the S phase cell population.
Sci Rep. 2023 Mar 20;13(1):4583.
Navtemadlin 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Non-small cell lung cancer patient-derived xenograft models (PDXs)
Oral
45 mg/kg
Once daily, 5 days/week for 3 weeks
To evaluate the anti-tumor activity of KRT-232 alone and in combination with trametinib in KRAS-mutant NSCLC PDX models. Results showed that the tumor regression rate after single agent therapy with KRT-232 was 11%, and it increased to 23% when combined with trametinib.
Am J Cancer Res. 2020 Dec 1;10(12):4464-4475
NSG mice
EBV-positive B-cell lymphoma xenograft model
Oral
45 mg/kg
Once daily, 5 days per week for 3 weeks
Navtemadlin significantly inhibited the growth of EBV-positive B-cell lymphoma and induced tumor regression
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