1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. BDTX-189

BDTX-189 

Cat. No.: HY-136789
Handling Instructions

BDTX-189 is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, includes EGFR/HER2 exon 20 insertion mutants. BDTX-189 shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity.

For research use only. We do not sell to patients.

BDTX-189 Chemical Structure

BDTX-189 Chemical Structure

CAS No. : 2414572-47-5

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Description

BDTX-189 is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, includes EGFR/HER2 exon 20 insertion mutants. BDTX-189 shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity[1].

IC50 & Target[1]

EGFR

0.2 nM (Kd)

HER2

0.76 nM (Kd)

RIPK2

1.2 nM (Kd)

BLK

13 nM (Kd)

In Vitro

BDTX-189 is a masterKey inhibitor of the ERBB allosteric mutant oncogene family with antiproliferative activity (IC50<100 nM for ERBB allosteric mutant oncogene family)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BDTX-189 (0-100 mg/kg; p.o.; daily for 15 dyas) shows dose-dependent tumor growth inhibition and regression in in athymic nude mice bearing HER2 S310F Ba/F3 allograft tumors[1].
BDTX-189 (1-50 mg/kg.p.o.; daily for 15 days) shows dose-dependent tumor growth inhibition and regression in athymic nude mice bearing CUTO-14 PDX tumors that express the EGFR mutation EGFR ASV[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

561.03

Formula

C₂₉H₂₉ClN₆O₄

CAS No.

2414572-47-5

SMILES

C=CC(NC1=CC2=C(NC3=CC=C(OCC4=NC=CC=C4)C(Cl)=C3)N=CN=C2C=C1OCCN5CCOCC5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

BDTX-189BDTX189BDTX 189EGFREpidermal growth factor receptorErbB-1HER1allostericoralinsertionmutantsoncogene athymicnudemiceBa/F3Inhibitorinhibitorinhibit

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