TM471-1

TM471-1 is an orally active and covalent Bruton's tyrosine kinase (BTK) inhibitor with IC50 values of 1.3 nM (BTKWT), >40,000 nM (BTKC481S), 7.9 nM (TEC) and 12.4 nM (TXK) . TM471-1 inhibits cell growth in vivo and in vitro, arrests cell cycle at G0/G1 phase and induces cell apoptosis[1].

Product Specifications

CAS Number

[2649008-95-5]

UNSPSC

12352005

Target

Apoptosis; Btk

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Smiles

O=C(N)C1=C(C2=CC=C(OC3=CC=CC=C3)C=C2)N=C4N1NCC[C@H]4C5CCN(C(C=C)=O)CC5

Molecular Formula

C27H29N5O3

Molecular Weight

471.55

References & Citations

[1]Zhang D, et al. Discovery of Imidazo[1,2-b]pyridazine Derivatives as Potent and Highly Selective Irreversible Bruton's Tyrosine Kinase (BTK) Inhibitors. J Med Chem. 2025 Jun 12;68 (11) :10897-10929.