2. Antibody-drug Conjugate/ADC Related
  3. ADC Cytotoxin
  4. Akt/ROCK-IN-1

Akt/ROCK-IN-1 (B12) 是 Akt 和 ROCK 的双重抑制剂，IC50 分别为 0.023 nM 和 1.47 nM。 AKT/Rock-In-1 具有神经母细胞瘤的抗肿瘤活性。

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Akt/ROCK-IN-1 Chemical Structure

Akt/ROCK-IN-1 Chemical Structure

CAS No. : 2983889-44-5

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Akt/ROCK-IN-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

体外研究
(In Vitro)

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[1]。
Akt/ROCK-IN-1 (800 nM ) 导致 Neuro2a 细胞显著增加在 G0/G1 期的细胞比例[1]。
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[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Akt/ROCK-IN-1 相关抗体:
体内研究
(In Vivo)

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[1]。
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[1]。

Pharmacokinetic Analysis in ICR mice Model[1]

药代动力学分析[1]

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: mice were implanted with Neuro2a cells[1]
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[1]
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.
分子量

509.37

Formula

C21H19BrF2N4O2S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Akt/ROCK-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Akt/ROCK-IN-12983889-44-5ADC CytotoxinADC PayloadAkt/ROCK InhibitorNeurological DiseaseInhibitorinhibitorinhibit

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目录号：
HY-156796
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