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Borussertib Akt inhibitor

Cat.No.S8839

Borussertib is a covalent-allosteric inhibitor of protein kinase Akt with an IC50 of 0.8 nM and a Ki of 2.2 nM for WT Akt.
Borussertib Akt inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 596.68

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Quality Control

Batch: S883901 DMSO]11 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.11%
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99.11

Solubility

In vitro
Batch:

DMSO : 11 mg/mL (18.43 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 596.68 Formula

C36H32N6O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1800070-77-2 -- Storage of Stock Solutions

Synonyms N/A Smiles C=CC(=O)NC1=CC2=C(C=C1)NC(=O)N2C3CCN(CC3)CC4=CC=C(C=C4)C5=C(C=C6C(=N5)C=CNC6=O)C7=CC=CC=C7

Mechanism of Action

Targets/IC50/Ki
Akt
(Cell-free assay)
0.8 nM
In vitro

Borussertib exhibits excellent cellular activity in the nanomolar range. The EC50 values (cell viability assay) of this compound in AN3CA, T47D, ZR-75-1, MCF-7, BT-474 and KU-19-19 cells are 191 nM, 48 nM, 5 nM, 277 nM, 373 nM and 7770 nM, respectively. It specifically binds to two non-catalytic cysteines in AKT at positions 296 and 310 by decorating allosteric ligands with electrophilic warheads at suitable positions, thus enabling the irreversible stabilization of the inactive conformation. This chemical potently inhibits proliferation of PI3K/PTEN-mutated cell lines.
In vivo

Borussertib reveals a good pharmacokinetic profile with reasonable microsomal stability in human and murine microsomes. PK studies are carried out in mice (2 mg/kg intravenous; 20 mg/kg oral gavage; 20 mg/kg, intraperitoneal), Despite a rather low oral bioavailability (<5%), reaching only a maximum plasma concentration of 78 ng/mL (0.13 µM), There is a significantly higher bioavailability upon intraperitoneal administration (39.6%), with maximum plasma levels of 683 ng/mL (1.14 µM).
References

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