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Akt1&PKA-IN-1 

Cat. No. M31261
Akt1&PKA-IN-1  Structure
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Biological Activity

Akt1&PKA-IN-1 is a potent dual Akt/PKA inhibitor with IC50 values of 0.03 , 0.11 μM, and 9.8 μM for PKAa, Akt, and CDK2, respectively. Akt1&PKA-IN-1 is selective for cyclin-dependent kinase 2 (CDK2).

Chemical Information
Molecular Weight 386.27
Formula C20H17Cl2N3O
CAS Number 1334107-58-2
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Shuang Wang, et al. Cell Oncol (Dordr). PKMYT1 inhibits lung adenocarcinoma progression by abrogating AKT1 activity

[2] Xueli Tian, et al. Mol Cancer. Costunolide is a dual inhibitor of MEK1 and AKT1/2 that overcomes osimertinib resistance in lung cancer

[3] Bijesh George, et al. Cells. AKT1 Transcriptomic Landscape in Breast Cancer Cells

[4] Qi-Dong Xia, et al. Cell Prolif. Network pharmacology and molecular docking analyses on Lianhua Qingwen capsule indicate Akt1 is a potential target to treat and prevent COVID-19

[5] Cameron Herberts, et al. Eur Urol. Activating AKT1 and PIK3CA Mutations in Metastatic Castration-Resistant Prostate Cancer

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Keywords: Akt1&PKA-IN-1  supplier, Akt, inhibitors, activators


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