DNA-PK-IN-13,3036751-03-5

DNA-PK-IN-13 产品活性：DNA-PK-IN-13 (Compound SK10) 是 DNA-PK 抑制剂，表现出极强的抑制活性 (IC50= 0.11 nM)。DNA-PK-IN-13 通过降低 γH2A.X 的表达水平和增强肿瘤细胞对化疗药物的敏感性，调节肿瘤细胞的增殖。DNA-PK-IN-13 具适用于肿瘤学研究。 产品来源： www.medchemexpress.cn/dna-pk-in-13.html 研究领域：Cell Cycle/DNA Damage | PI3K/Akt/mTOR 作用靶点：DNA-PK In Vitro: DNA-PK-IN-13 displays the best antiproliferative activities with IC50 values of 0.6 μM against Jurkat T-cell. DNA-PK-IN-13 (0.1-40 μM; 10 min) concentration-dependently decreases the expression level of γH2A.X in Jurkat cells and HepG2 cells. DNA-PK-IN-13 (1 μM; 24 hours) in combination with doxorubicin (HY-15142A) (0.1 μM) results in a significant decrease in the proportion of S-phase and an increase in the proportion of G2/M-phase in the Jurkat cell. In Vivo: DNA-PK-IN-13 has good oral bioavailability (F = 31.8%). Pharmacokinetic Analysis in DNA-PK-IN-13 Route Dose (mg/kg) AUC0-t (ug/L·h) AUC0−∞ (ug/L·h) t1/2 (h) Tmax (h) Cl (L/h/kg) Vz (L/kg) C0 (ug/L) Cmax (ug/L) F (%) i.v. 2 604.4 ± 61.6 605.4 ± 61.9 1.0 ± 0.4 0.083 3.3 ± 0.3 4.7 ± 1.9 1003.9 ± 201.8 NA / p.o. 10 949.5 ± 405.2 962.3 ± 412.1 2.0 ± 0.6 1.4 ± 1.1 12.6 ± 7.4 38.8 ± 30.2 NA 324.1 ± 149.0 31.8 DNA-PK-IN-13 (i.p.; 10 mg/kg; single dose) has tumor suppressor activity in CT26 colon cancer mice.Co-administration with doxorubicin (2.5 mg/kg) is effective and safe. DNA-PK-IN-13 (i.p.; 10 mg/kg; 13 consecutive days) in combination with PD-1/PD-L1 inhibitors inhibits tumor growth more significantly. 相关产品：LY294002 | AZD-7648 | KU-57788 | Torin 2 | PI-103 | Nedisertib | STL127705 | NU 7026 | PIK-90 | Samotolisib | VX-984 | PIK-75 hydrochloride | CC-115 | KU-0060648 | BAY-8400 | LTURM34 | ETP-45658 | YU238259 | SF2523 | (R)-VX-984 | Compound 401 | AMA-37 | ATR-IN-15 | Canfosfamide | DNA-PK-IN-1 | DNA-PK-IN-10 | DNA-PK-IN-11 | DNA-PK-IN-12