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Chemical Structure : TAS-121
Catalog No.: PC-38346Not For Human Use, Lab Use Only.
TAS-121 (TAS 121) is an orally available, potent, novel third-generation EGFR-TKI that selectively targets EGFR activating and T790M resistance mutations, sparing wild-type EGFR.
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TAS-121 (TAS 121) is an orally available, potent, novel third-generation EGFR-TKI that selectively targets EGFR activating and T790M resistance mutations, sparing wild-type EGFR.
TAS-121 inhibited the L858R mutation and Ex19del mutation of EGFR with IC50 values of 1.7 and 2.7 nM, respectively.
TAS-121 also inhibited the L858R/T790M mutation and Ex19del/T790M mutation with IC50 values of 0.56 and 1.1 nM, inhibits wild-type EGFR with IC50 of 8.2 nM.
TAS-121 potently inhibited the growth of HCC827 cells (EGFR Ex19del) and NCI-H1975 cells (EGFR L858R, T790M), with IC50 values of 3.8 and 30 nM, respectively.
TAS-121 (50 and 100 mg/kg) showed potent dose-dependent activity against NCI-H1975 tumors, and regression of lesions in NCI-H1975 xenograft models, also showed antitumor activity in an HCC827 xenograft model at doses from 6.3 to 25 mg/kg.
TAS-121 (25 to 100 mg/kg) showed antitumor activity in an SW48 xenograft model harboring an EGFR G719S mutation.
| M.Wt | 384.443 | |
| Formula | C22H20N6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Nishio M, et al. Invest New Drugs. 2019 Dec;37(6):1207-1217.
2. Ito K, et al. Mol Cancer Ther. 2019 May;18(5):920-928.
3. Watanabe S, et al. Thorac Cancer. 2021 Mar;12(5):631-642.
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