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编 号：F762701
分子式：C21H19BrF2N4O2S
分子量：509.37
分子式：C21H19BrF2N4O2S
分子量：509.37
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CAS No: 2983889-44-5
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生物活性：
Akt/ROCK-IN-1 (B12) is a dual inhibitor for Akt and ROCK, with the IC50s of 0.023 nM and 1.47 nM, respectively. Akt/ROCK-IN-1 has antitumor activity for neuroblastoma.
体内研究：
Akt/ROCK-IN-1 (20, 40 mg/kg; i.p.; 每天注射持续14天) 可抑制植入 Neuro2a 细胞的小鼠的肿瘤生长。Akt/ROCK-IN-1 (10 mg/kg; i.p., p.o.单剂量) 与口服给药相比，腹腔注射在大鼠体内产生更好的药代动力学参数。Pharmacokinetic Analysis in ICR mice Model 药代动力学分析Route Dose (mg/kg) Tmax (h)T1/2 (h) Cmax (ng/mL) Cl (mL·h/kg)AUC0-t (ng·h/mL) AUC0-∞ (ng·h/mL) MRT (h) Vss/Vd (L/kg)
p.o. 10 2.0 4.3 96.3 15374.1 481.8 650.4 6.2 96
i.p. 10 0.3 2.2 561.3 5934.9 1548.9 1685.0 3.2 19.0
Animal Model:mice were implanted with Neuro2a cells
Dosage:20 mg/kg and 40 mg/kg; everyday for 14d
Administration:i.p
Result:Inhibited tumor growth compared to the vehicle control.Mice maintained stable body weights throughout the treatment, indicating a favorable safety profile. Post-treatment analysis showed significant differentiation in tumor cells, demonstrated by increased expression of differentiation markers.
Animal Model:SD rats or ICR mice
Dosage:10 mg/kg; Single Dose
Administration:i.p.; p.o.
Result:Showed low oral bioavailability and plasma stability, particularly in rat liver microsomes with only 18.0% remaining after 1 hour.Intraperitoneal administration resulted in better pharmacokinetic parameters compared to oral administration, suggesting that this route could be more suitable for achieving therapeutic plasma concentrations.
体外研究：
Akt/ROCK-IN-1 (0.5 μM;0-72 h ) 在 Neuro2a 细胞中显示出强大的抗增殖效应和出色的分化诱导活动。Akt/ROCK-IN-1 (800 nM ) 导致 Neuro2a 细胞显著增加在 G0/G1 期的细胞比例。Akt/ROCK-IN-1 (0.5, 2 μM) 导致 mTOR, GSK-3β 和 PRAS40 的磷酸化水平显著下降，而 Akt 的磷酸化水平则表现出反馈性增加。
Akt/ROCK-IN-1 (B12) is a dual inhibitor for Akt and ROCK, with the IC50s of 0.023 nM and 1.47 nM, respectively. Akt/ROCK-IN-1 has antitumor activity for neuroblastoma.
体内研究：
Akt/ROCK-IN-1 (20, 40 mg/kg; i.p.; 每天注射持续14天) 可抑制植入 Neuro2a 细胞的小鼠的肿瘤生长。Akt/ROCK-IN-1 (10 mg/kg; i.p., p.o.单剂量) 与口服给药相比，腹腔注射在大鼠体内产生更好的药代动力学参数。Pharmacokinetic Analysis in ICR mice Model 药代动力学分析Route Dose (mg/kg) Tmax (h)T1/2 (h) Cmax (ng/mL) Cl (mL·h/kg)AUC0-t (ng·h/mL) AUC0-∞ (ng·h/mL) MRT (h) Vss/Vd (L/kg)
p.o. 10 2.0 4.3 96.3 15374.1 481.8 650.4 6.2 96
i.p. 10 0.3 2.2 561.3 5934.9 1548.9 1685.0 3.2 19.0
Animal Model:mice were implanted with Neuro2a cells
Dosage:20 mg/kg and 40 mg/kg; everyday for 14d
Administration:i.p
Result:Inhibited tumor growth compared to the vehicle control.Mice maintained stable body weights throughout the treatment, indicating a favorable safety profile. Post-treatment analysis showed significant differentiation in tumor cells, demonstrated by increased expression of differentiation markers.
Animal Model:SD rats or ICR mice
Dosage:10 mg/kg; Single Dose
Administration:i.p.; p.o.
Result:Showed low oral bioavailability and plasma stability, particularly in rat liver microsomes with only 18.0% remaining after 1 hour.Intraperitoneal administration resulted in better pharmacokinetic parameters compared to oral administration, suggesting that this route could be more suitable for achieving therapeutic plasma concentrations.
体外研究：
Akt/ROCK-IN-1 (0.5 μM;0-72 h ) 在 Neuro2a 细胞中显示出强大的抗增殖效应和出色的分化诱导活动。Akt/ROCK-IN-1 (800 nM ) 导致 Neuro2a 细胞显著增加在 G0/G1 期的细胞比例。Akt/ROCK-IN-1 (0.5, 2 μM) 导致 mTOR, GSK-3β 和 PRAS40 的磷酸化水平显著下降，而 Akt 的磷酸化水平则表现出反馈性增加。
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