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.
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- CAS. Nr.: 2758034-98-7
- Formel: C32H34N6O6
- Molecular Weight:598.65
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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. Nr. 2758034-98-7
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Molecular Weight 598.65
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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