| Identification | Back Directory | [Name]
BDTX-189 | [CAS]
2414572-47-5 | [Synonyms]
BDTX-189
2-Propenamide, N-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-7-[2-(4-morpholinyl)ethoxy]-6-quinazolinyl]- | [Molecular Formula]
C29H29ClN6O4 | [MDL Number]
MFCD32878264 | [MOL File]
2414572-47-5.mol | [Molecular Weight]
561.03 |
| Chemical Properties | Back Directory | [Boiling point ]
778.0±60.0 °C(Predicted) | [density ]
1.349±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:22.56(Max Conc. mg/mL);40.21(Max Conc. mM)
DMF:1.0(Max Conc. mg/mL);1.78(Max Conc. mM)
DMF:PBS (pH 7.2) (1:2):0.3(Max Conc. mg/mL);0.53(Max Conc. mM) | [form ]
A solid | [pka]
12.20±0.43(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
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[1]. | [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[1].
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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[1]. | [IC 50]
EGFR: 0.2 nM (Kd); HER2: 0.76 nM (Kd); RIPK2: 1.2 nM (Kd); BLK: 13 nM (Kd) | [References]
[1] Elizabeth Buck, et al. BDTX-189, a Potent and Selective Inhibitor of Allosteric EGFR and HER2 Oncogenic Mutations. |
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