BDTX-189 free base · Synonyms: Tuxobertinib

Tuxobertinib is a potent, orally active and selective inhibitor of allosteric EGFR.

For research use only. Not for human or veterinary use.

Target EGFR

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

BDTX-189 structure

CAS No.: 2414572-47-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
5 g	USD 780.00	BP-02010-5g	In stock	Get quote
10 g	USD 1,380.00	BP-02010-10g	In stock	Get quote

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Description

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

Biological activity

In Vitro Tuxobertinib is a masterKey inhibitor of the ERBB allosteric mutant oncogene family with antiproliferative activity (IC50<100 nM for ERBB allosteric mutant oncogene family). In Vivo Tuxobertinib (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. ? Tuxobertinib (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.

Identifiers

SMILES: C=CC(NC1=CC2=C(NC3=CC=C(OCC4=NC=CC=C4)C(Cl)=C3)N=CN=C2C=C1OCCN5CCOCC5)=O
InChIKey: HIBPKFXWOPYJPZ-UHFFFAOYSA-N

Specifications

MW (average): 561.0310
Formula: C₂₉H₂₉ClN₆O₄
CAS No.: 2414572-47-5
Physical state: Solid
Color: Off-white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Elizabeth Buck, et al. BDTX-189, a Potent and Selective Inhibitor of Allosteric EGFR and HER2 Oncogenic Mutations.

Same target

Search EGFR

Same research area

Search Cancer