ASP3026 is a potent, selective, and orally administered inhibitor of anaplastic lymphoma kinase (ALK). It promotes apoptosis in tumor cells and is applicable in non-small cell lung cancer (NSCLC) research[1][2].
To evaluate the effect of ASP3026 on the viability of NPM-ALK+ ALCL cells. Results showed that ASP3026 significantly reduced the viability of all tested cell lines at 48 and 72 hours, with varying IC50 values across cell lines.
Oncotarget. 2014 Jul 30;5(14):5750-63.
Ba/F3 NPM-ALK S1206Y
0.110 µmol/L
72 hours
Evaluate the inhibitory activity of ASP3026 on NPM-ALK S1206Y mutant cells, IC50 was 0.110 µmol/L, showing sensitivity.
Cancer Med. 2015 Jul;4(7):953-65.
Ba/F3 NPM-ALK G1269A
0.364 µmol/L
72 hours
Evaluate the inhibitory activity of ASP3026 on NPM-ALK G1269A mutant cells, IC50 was 0.364 µmol/L, showing resistance.
Cancer Med. 2015 Jul;4(7):953-65.
Ba/F3 NPM-ALK G1202R
1.177 µmol/L
72 hours
Evaluate the inhibitory activity of ASP3026 on NPM-ALK G1202R mutant cells, IC50 was 1.177 µmol/L, showing high resistance.
Cancer Med. 2015 Jul;4(7):953-65.
Ba/F3 NPM-ALK L1152R
2.763 µmol/L
72 hours
Evaluate the inhibitory activity of ASP3026 on NPM-ALK L1152R mutant cells, IC50 was 2.763 µmol/L, showing high resistance.
Cancer Med. 2015 Jul;4(7):953-65.
Ba/F3 NPM-ALK L1196M
0.682 µmol/L
72 hours
Evaluate the inhibitory activity of ASP3026 on NPM-ALK L1196M mutant cells, IC50 was 0.682 µmol/L, showing resistance.
Cancer Med. 2015 Jul;4(7):953-65.
Ba/F3 NPM-ALK C1156Y
0.284 µmol/L
72 hours
Evaluate the inhibitory activity of ASP3026 on NPM-ALK C1156Y mutant cells, IC50 was 0.284 µmol/L, showing moderate resistance.
Cancer Med. 2015 Jul;4(7):953-65.
Ba/F3 NPM-ALK WT
0.084 µmol/L
72 hours
Evaluate the inhibitory activity of ASP3026 on NPM-ALK WT cells, IC50 was 0.084 µmol/L.
Cancer Med. 2015 Jul;4(7):953-65.
Human hepatocyte carcinoma HepG2 cells
0-300 μM
72 hours
To assess the cytotoxicity of ASP3026 analogues, compound 36 showed low toxicity.
Commun Biol. 2024 Jun 18;7(1):742.
Plasmodium falciparum 3D7 parasites
10 μM
72 hours
To evaluate the inhibitory effects of ASP3026 analogues on Plasmodium growth, compound 36 showed the most potent inhibition with an EC50 value of 736 nM.
Commun Biol. 2024 Jun 18;7(1):742.
Plasmodium falciparum 3D7
5.61 ± 0.26 µM
72 hours
To evaluate the inhibitory effect of ASP3026 on Plasmodium growth, results showed that ASP3026 effectively inhibited Plasmodium growth.
Nucleic Acids Res. 2020 Nov 18;48(20):11566-11576.
ASP3026 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
SCID Beige mice
Crizotinib-resistant PDX mouse model
Oral
100 mg/kg/day
Once daily for approximately 2 weeks
Evaluate the effect of ASP3026 on tumor growth in crizotinib-resistant PDX mice, results showed significant tumor growth inhibition
iScience. 2024 Aug 30;27(9):110846
C.B-17 SCID mice
Systemic xenograft lymphoma model
Oral gavage
30 mg/kg
Daily administration for 10 weeks (uninterrupted group) or 2 weeks followed by 4 weeks interruption and then 4 weeks continuation (interrupted group)
To evaluate the inhibitory effect of ASP3026 on systemic NPM-ALK+ ALCL growth. Results showed that mice in the uninterrupted group achieved complete remission with no relapse or lymphoma-related death, while mice in the interrupted group experienced rapid relapse after discontinuation but showed significant tumor regression upon resumption of treatment.
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