TX2-121-1

• Description :

  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) ) [1].

• CAS Number :

  [1603845-42-6]

• UNSPSC :

  12352005

• Target :

  Akt; EGFR; ERK; PROTACs

• Type :

  Reference compound

• Related Pathways :

  JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; PROTAC; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/tx2-121-1.html

• Solubility :

  10 mM in DMSO

• 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

• Molecular Formula :

  C42H52N8O3

• Molecular Weight :

  716.91

• References & Citations :

  [1]Lim SM, et, al. Development of small molecules targeting the pseudokinase Her3. Bioorg Med Chem Lett. 2015 Aug 15;25 (16) :3382-9.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 3

• Isoform :

  ErbB3/HER3