TX2-121-1
TX2-121-1 is a potent and selective Her3 (ErbB3) degrader that contains a hydrophobic adamantane moiety. TX2-121-1 has an IC50 of 49 nM for Her3. TX2-121-1 inhibits Her3-dependent signaling and heterodimerization of Her3. TX2-121-1 has the ability to inhibit cell proliferation. TX2-121-1 can be used in the study of tumors. (Pink: Her3 inhibitor (HY-164988); Black: Linker; Blue: Adamantane (HY-N2427)).
(Pink: HER3 ligand (HY-164988); Blue: hyt ligand (HY-N2427); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 1603845-42-6
- Formula: C42H52N8O3
- Molecular Weight:716.91
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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
Biological Activity
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HER3 49 nM (IC50) |
TX2-121-1 (1-5 μM; 12 h) induces Her3 degradation, inhibits the phosphorylation of downstream Erk and Akt and cell proliferation in PC9 GR4 cells[1].
TX2-121-1 (1 μM; 6 h) interferes with the heterodimerization of Her3 with Her2 and c-Met in PC9 GR4 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC9 GR4 cells
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Concentration:1 and 5 μM
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Incubation Time:12 h
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Result:Significantly inhibited the level of Her3.
Inhibited the phosphorylation levels of Erk and Akt.
Chemical Information
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CAS No. 1603845-42-6
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Molecular Weight 716.91
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Formula C42H52N8O3
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SMILES
C[C@@H](C(NCCN1CCC(N2C3=NC=NC(N)=C3C(C(C=C4)=CC(NC(C=C)=O)=C4OC5=CC=CC=C5)=N2)CC1)=O)CCC6(C[C@H](C7)C8)C[C@H]8C[C@H]7C6
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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
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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