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Chemical Structure : TX1-85-1
CAS No.: 1603845-32-4
Catalog No.: PC-38536Not For Human Use, Lab Use Only.
TX1-85-1 is a potent, selective, irreversible and covalent inhibitor of pseudokinase Her3 (ErbB3) with IC50 of 23 nM in FRET-based binding assay.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $188 | In stock | |
| 10 mg | $298 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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TX1-85-1 is a potent, selective, irreversible and covalent inhibitor of pseudokinase Her3 (ErbB3) with IC50 of 23 nM in FRET-based binding assay.
TX1-85-1 covalently modifies Cys721 of Her3 in vitro and in cells.
TX1-85-1 is insufficient to inactivate the Her3/PI3K/AKT pathway explaining lack of growth inhibition for Her3 dependent cells.
TX1-85-1 arrested cell proliferation, inhibited the in vitro tumorigenicity, and lead to loss of stemness in the conversion of induced pluripotent stem cells (iPSCs) into cancer stem cells (CSCs).
| M.Wt | 580.693 | |
| Formula | C32H36N8O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-(5-(1-(4-(4-Acetylpiperazin-1-yl)cyclohexyl)-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-phenoxyphenyl)acrylamide |
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1. Xie T, et al. Nat Chem Biol. 2014 Dec;10(12):1006-12.
2. Lim SM, et al. Bioorg Med Chem Lett. 2015 Aug 15;25(16):3382-9.
3. Hassan G, et al. Sci Rep. 2022 Feb 17;12(1):2711.
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