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.
For research use only. We do not sell to patients.
- CAS No.: 2758034-98-7
- Formula: C32H34N6O6
- Molecular Weight:598.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
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.
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Cell Line:SK-BR-3 cells
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Concentration:10 nM, 30 nM, 100 nM
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Incubation Time:3 h and 48 h
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Result:Inhibited the phosphorylation of HER2, HER3, AKT, and ERK.
PK parameters of TAS2940 after a single oral administration or multiple oral administrations for 7 days in male BALB/cAJcl-nu/nu mice[1].
| Administration | Dose (mg/kg) | Tmax (h) | Apparent T1/2 (h) | Cmax (ng/mL) | AUClast (ng▪h/mL) |
| Single administration | 6.25 | 0.33±0.14 | 2.15±2.15 | 601±111 | 795±229 |
| Single administration | 12.5 | 0.25±0.00 | NC | 1590±220 | 2010±230 |
| Single administration | 25 | 0.25±0.00 | 2.09 | 3580±190 | 5080±820 |
| Repeated administrations for 7 days | 6.25 | 0.25±0.00 | 2.20±2.73 | 1170±300 | 972±239 |
| Repeated administrations for 7 days | 12.5 | 0.33±0.14 | 0.69 | 2040±230 | 2800±460 |
| Repeated administrations for 7 days | 25 | 0.42±0.14 | 0.76 | 3710±360 | 6180±310 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-week-old male BALB/cAJcl-nu/nu mice injected with NCI-N87, MCF10A_HER2/insYVMA_v, or NCI-H1975 EGFR D770_N771insSVD cellsMCF10A_HER2/insYVMA_v[1]
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Dosage:3.1-25 mg/kg (0.5 w/v% HPMC)
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Administration:po; once daily; for 14 days
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Result:Inhibited tumor growth in xenograft mouse models.
Chemical Information
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CAS No. 2758034-98-7
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Molecular Weight 598.65
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Formula C32H34N6O6
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SMILES
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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TAS2940 fumarate Related Classifications
HY-153856A Related Classifications
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