Borussertib

Catalog No.S8839 Batch:S883901

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Technical Data

Formula

C36H32N6O3
Molecular Weight 596.68 CAS No. 1800070-77-2
Solubility (25°C)* In vitro DMSO 11 mg/mL (18.43 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
0.28mg/ml Taking the 1 mL working solution as an example, add 50 μL of 5.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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].
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].

Protocol (from reference)

Cell Assay:

[2]
  • 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

    --
Animal Study:

[2]
  • 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

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.