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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 ; Black: Linker; Blue: Adamantane (HY-N2427) ).

Product Specifications

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

Frequently Asked Questions

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