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].

• 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

• CAS Number:

  1603845-42-6