TAS2940 fumarate 

TAS2940 fumarate is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 fumarate against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC₅₀ values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 fumarate can be used for the study of tumors with HER2 and EGFR aberrations^[1].

TAS2940 fumarate (10-100 nM; 3-48 h) markedly increases the protein levels of B-cell lymphoma 2 interacting mediator of cell death (BIM) and cleaved PARP. TAS2940 fumarate inhibits the phosphorylation of HER2, HER3, and their downstream proteins, AKT and ERK^[1].
TAS2940 fumarate inhibits MCF10A_HER2, MCF10A_HER2/S310F, MCF10A_HER2/L755S, MCF10A_HER2/V777L, MCF10A_HER2/V842I, MCF10A_HER2/insYVMA, MCF10A_EGFR, MCF10A_EGFR (EGF+), MCF10A_EGFR/V769_D770insASV, and MCF10A_EGFR/D770_N771insSVD cells ,with IC₅₀ values of 2.27 nM, 1.98 nM, 3.74 nM, 1.54 nM, 3.28 nM, 1.91 nM, 9.38 nM, 0.804 nM, 5.64 nM, and 2.98 nM, respectively^[1].

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

TAS2940 fumarate (3.1-25 mg/kg; po; once daily; for 14 days) inhibits tumor growth in xenograft mouse models with ERBB aberrations: HER2 amplification, HER2/EGFR exon 20 insertions, and EGFR vIII mutation^[1].
PK parameters of TAS2940 after a single oral administration or multiple oral administrations for 7 days in male BALB/cAJcl-nu/nu mice^[1].

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

598.65

C₃₂H₃₄N₆O₆

2758034-98-7

OC(/C=C/C(O)=O)=O.NC1=NC=NC2=C1C(C(N[C@@H](C3=CC=CC=C3)C)=O)=C(C#CC4CC4)N2[C@@H]5C[C@H](C)N(C(C=C)=O)C5

Room temperature in continental US; may vary elsewhere.

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

• [1]. Kei Oguchi, et al. TAS2940, a novel brain-penetrable pan-ERBB inhibitor, for tumors with HER2 and EGFR aberrations. Cancer Sci. 2023 Feb;114(2):654-664.  [Content Brief]