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CAS No. :
MCE 国际站:DDO-2728
产品活性:DDO-2728 (化合物 19) 是一种选择性 AlkB homologue 5 (ALKBH5) 抑制剂,其 IC50 为 2.97 μM。DDO-2728 增加 N6 methyladenosine (m6A) 修饰的丰度,诱导细胞凋亡和细胞周期阻滞。DDO-2728 在 MV4−11 异种移植模型中抑制肿瘤生长且具有良好的安全性,显示出靶向 ALKBH5 在癌症研究中的潜力。
研究领域:Protein Tyrosine Kinase/RTK | Apoptosis
作用靶点:Anaplastic lymphoma kinase (ALK) | Apoptosis
In Vitro: DDO-2728 (0-40 μM, 48 h) increases m6A methylation levels in the MOLM-13, HEK293and MV4−11 cells over a concentration gradient.
DDO-2728 (0.01-100 μM, 72 h) inhibits the proliferation of MOLM-13 and MV4−11 cells with IC50s of 0.45 and 1.2 μM respectively, and showes a relatively weak toxicity in HEK293 and HUVECs.
DDO-2728 (20 μM, 48 h) significantly arrests the cell cycle of MOLM-13 and MV4−11 cells at the G1/M phase.
DDO-2728 (5, 10 μM, 48 h) concentration-dependently induces cell apoptosis of MV4−11 and MOLM-13 cells.
DDO-2728 (20 μM, 24 h) decreases the half-lives of TACC3 mRNA in MOLM-13 and MV4−11 cells.
DDO-2728 (0-10 μM, 48 h) significantly reduces the abundance of TACC3 and c-Myc in MOLM-13 and MV4−11 cells at both mRNA and protein levels.
1.19
Metabolic Stability in Rat and Human Plasma and Liver Microsomes
Species |
Plasma T1/2 (min) |
Microsome T1/2 (min) |
Microsome CL (μL/min/mg) |
Human |
624 |
430 |
3.2 |
Rat |
251 |
13.8 |
100.4 |
In Vivo: DDO-2728 (10-40 mg/kg, i.p., daily for 14 d) effectively inhibits tumor growth in MV4−11 xenograft nude mice..
1.19
Pharmacokinetic Parameters of DDO-2728 in Rats
Parameter |
Rat (i.v., 2mg/kg) |
Rat (i.p., 10mg/kg) |
T1/2 (min) |
36.7 ± 3.2 |
148.3 ± 4.6 |
Cmax (ng/mL) |
13388.3 ± 784.5 |
2337.5 ± 295.7 |
Tmax (min) |
30 |
AUC0-∞ (min·μg/mL) |
404.3 ± 58.6 |
349.1 ± 26.1 |
Vz_F_obs (mL/kg) |
263.6 ± 17.5 |
6177.6 ± 650.2 |
Cl_F_obs (mL/min/kg) |
5.0 ± 0.5 |
28.8 ± 2.2 |
MRT (min) |
77.8 ± 15.5 |
168.2 ± 1.2 |
F (%) |
17.3 |
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