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

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.

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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 Related Antibodies

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Description

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].

In Vitro

Akt/ROCK-IN-1 (0.5 μM; 0-72 h ), shows potent antiproliferative effects and excellent differentiation-inducing activity in Neuro2a cells.[1].
Akt/ROCK-IN-1 (800 nM ) can lead to a significant increase in the proportion of Neuro2a cells in G0/G1 phase[1].
Akt/ROCK-IN-1 (0.5, 2 μM) can lead to a significant decrease in the phosphorylation levels of mTOR, GSK-3β, and PRAS40, whereas Akt showed a feedback increase in phosphorylation levels[1].

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

Akt/ROCK-IN-1 Related Antibodies
In Vivo

Akt/ROCK-IN-1 (20, 40 mg/kg; i.p.; everyday for 14d) can inhibit tumor growth in mice are implanted with Neuro2a cells[1].
Akt/ROCK-IN-1 (10 mg/kg; i.p., p.o.; Single Dose) with intraperitoneal administration results in better pharmacokinetic parameters compared to oral administration in rats[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

MedChemExpress (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.
Molecular Weight

509.37

Formula

C21H19BrF2N4O2S
CAS No.
SMILES

O=C(C(S1)=CC2=C1OCCN3C2=C(Br)C=N3)N[C@@H]4CNCC[C@H]4C5=CC=C(F)C(F)=C5
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Akt/ROCK-IN-1 Related Classifications

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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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