Itacnosertib

Itacnosertib (TP-0184) is the inhibitor for FLT3, ACVR1 (ALK2, IC50=8 nM) and JAK2 (IC50=8540 nM) . Itacnosertib exhibits anti-leukemic activity[1][2].

Product Specifications

CAS Number

[1628870-27-8]

Product Name Alternative

TP-0184

UNSPSC

12352005

Target

Akt; Anaplastic lymphoma kinase (ALK) ; FLT3; JAK; mTOR; PI3K; STAT; TGF-beta/Smad; TGF-β Receptor

Type

Reference compound

Related Pathways

Epigenetics; JAK/STAT Signaling; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt; TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/itacnosertib.html

Purity

99.06

Solubility

DMSO : 12.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CN1CCN(C2=CC=C(NC3=NC=CC(NC4=CC=CN=C4C5=NC=CC=C5)=N3)C=C2OC)CC1

Molecular Formula

C26H28N8O

Molecular Weight

468.55

References & Citations

[1]Mollard, Alexis; Warner, Steven L.; Flynn, Gary A.; Vankayalapati, Hariprasad; Bearss, David J. Preparation of [ (piperazinylphenyl) amino]pyrimidine derivatives as JAK2 and ALK2 inhibitors. WO2014151871 A2|[2]Tyagi A, et al., TP-0184 inhibits FLT3/ACVR1 to overcome FLT3 inhibitor resistance and hinder AML growth synergistically with venetoclax. Leukemia. 2024 Jan;38 (1) :82-95.