Home Protein Tyrosine Kinase EGFR inhibitor - HER2 inhibitor - RIP kinase inhibitor Tuxobertinib (BDTX-189) For research use only.

Tuxobertinib (BDTX-189)

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.

Tuxobertinib (BDTX-189) Chemical Structure

Tuxobertinib (BDTX-189) Chemical Structure

CAS No. 2414572-47-5

Purity & Quality Control

Tuxobertinib (BDTX-189) Related Products

Signaling Pathway

EGFR Signaling Pathways

EGFR Signaling Pathway

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
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]
Cell Research Cell lines A431 cells, H292 cells
Concentrations --
Incubation Time 0-24 h
Method

--
In Vivo
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]
Animal Research Animal Models athymic nude mice
Dosages 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg, 50 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04209465 Terminated
Solid Tumor
Black Diamond Therapeutics Inc.
 December 19 2019 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 561.03 Formula

C29H29ClN6O4
CAS No. 2414572-47-5 SDF --
Smiles ClC1=C(OCC2=NC=CC=C2)C=CC(=C1)NC3=NC=NC4=C3C=C(NC(=O)C=C)C(=C4)OCCN5CCOCC5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 25 mg/mL ( (44.56 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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