Home PI3K/Akt/mTOR Akt inhibitor Borussertib For research use only.

Borussertib

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 Chemical Structure

Borussertib Chemical Structure

CAS: 1800070-77-2

Purity & Quality Control

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

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Biological Activity

Description 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.
Targets
Akt [1]
(Cell-free assay)
0.8 nM
In vitro
In vitro

Borussertib exhibits excellent cellular activity in the nanomolar range. The EC50 values (cell viability assay) of borussertib 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[1]. Borussertib 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. Borussertib potently inhibits proliferation of PI3K/PTEN-mutated cell lines[2].
Cell Research Cell lines Breast, bladder, pancreas, and endometrium cancer cell lines harboring genetic alterations in the PI3K/AKT and RAS/MAPK pathways
Concentrations 30 µM to 0.1 nM
Incubation Time 96 h
Method

--
In Vivo
In vivo

Borussertib reveals a good pharmacokinetic profile with reasonable microsomal stability in human and murine microsomes[1]. 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)[2].
Animal Research Animal Models RjOrl:SWISS mice (aged 8-10 weeks)
Dosages 20 mg/kg (Oral/IP); 2 mg/kg (IV)
Administration by oral gavage/intraperitoneal/IV

Chemical Information & Solubility

Molecular Weight 596.68 Formula

C36H32N6O3
CAS No. 1800070-77-2 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 11 mg/mL ( (18.43 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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