Tuxobertinib (BDTX-189)

Catalog No.S9786 Batch:S978601

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Technical Data

Formula

C29H29ClN6O4
Molecular Weight 561.03 CAS No. 2414572-47-5
Solubility (25°C)* In vitro DMSO 33 mg/mL (58.82 mM)
Water Insoluble
Ethanol Insoluble
* <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 1 publication

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.