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Borussertib

Cat. No. M20677
Borussertib Structure
Size Price Availability Quantity
5mg USD 330  USD330 In stock
10mg USD 500  USD500 In stock
25mg USD 900  USD900 In stock
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Quality Control & Documentation
Biological Activity

Borussertib is a first-in-class covalently-mutated inhibitor of the protein kinase Akt, with an IC50 value of 0.8 nM and a Ki value of 2.2 nM for Aktwt.

Chemical Information
Molecular Weight 596.68
Formula C36H32N6O3
CAS Number 1800070-77-2
Solubility (25°C) DMSO 100 mg/mL
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] Jrn Weisner, et al. Cancer Res. Preclinical Efficacy of Covalent-Allosteric AKT Inhibitor Borussertib in Combination with Trametinib in KRAS-Mutant Pancreatic and Colorectal Cancer

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Keywords: Borussertib supplier, Akt, inhibitors, activators


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