TAS2940
TAS2940 is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 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 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.: 2451398-65-3
- Formula: C28H30N6O2
- Molecular Weight:482.58
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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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Help & FAQs
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Biological Activity
TAS2940 (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 inhibits the phosphorylation of HER2, HER3, and their downstream proteins, AKT and ERK[1].
TAS2940 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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2451398-65-3
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Molecular Weight 482.58
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Formula C28H30N6O2
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SMILES
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
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Data Sheet (279 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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