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TX1-85-1 is an ErbB3 inhibitor with IC50 of 23 nM, it is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 possesses an anti-proliferation EC50s of 9.9, 11.5, and 16.9 μM for Ovcar8, HCC827 GR6, and PC9 GR4 cells, respectively. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.
| Molecular Weight | 580.68 |
| Formula | C32H36N8O3 |
| CAS Number | 1603845-32-4 |
| Solubility (25°C) | DMSO 3 mg/mL |
| Storage | -20°C, dry, sealed |
[2] Ting Xie, et al. Nat Chem Biol. Pharmacological targeting of the pseudokinase Her3
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