Tuxobertinib (BDTX-189)

Catalog No.S9786 Batch:S978602

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Technical Data

Formula

C29H29ClN6O4
Molecular Weight 561.03 CAS No. 2414572-47-5
Solubility (25°C)* In vitro DMSO 25 mg/mL (44.56 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.31mg/ml Taking the 1 mL working solution as an example, add 50 μL of 6.2 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. 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 Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity.
Targets
EGFR [1]
(Cell-free assay)		 HER2 [1]
(Cell-free assay)		 RIPK2 [1]
(Cell-free assay)		 BLK [1]
(Cell-free assay)
0.2 nM(Kd) 0.76 nM(Kd) 1.2 nM(Kd) 13 nM(Kd)
In vitro

BDTX-189 is a potent, selective, irreversible active site inhibitor of the ERBB allosteric mutant oncogene family. BDTX-189 achieves a superior selectivity profile in cell-based assays.[1]
In vivo

BDTX-189 is differentiated by potent, sustained inactivation of multiple allosteric ERBB mutants in vivo. BDTX-189 achieves dose-dependent regression of allosteric HER2 and EGFR tumors at well-tolerated doses.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    A431 cells, H292 cells

  • Concentrations

    --

  • Incubation Time

    0-24 h

  • Method

    --
Animal Study:

[1]
  • Animal Models

    athymic nude mice

  • Dosages

    1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg, 50 mg/kg

  • Administration

    Oral gavage

Selleck's Tuxobertinib (BDTX-189) has been cited by 3 publications

BDTX-189, a novel tyrosine kinase inhibitor, inhibits cell activity via ERK and AKT pathways in the EGFR C797S triple mutant cells [ Chem Biol Interact, 2024, 395:111033] PubMed: 38710274
Young and undamaged recombinant albumin alleviates T2DM by improving hepatic glycolysis through EGFR and protecting islet β cells in mice [ J Transl Med, 2023, 21(1):89] PubMed: 36747238
Young and undamaged recombinant albumin alleviates T2DM by improving hepatic glycolysis through EGFR and protecting islet β cells in mice [ J Transl Med, 2023, 21(1):89] PubMed: 36747238

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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.