T025

T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM) . T025 has an anti-tumor efficiency, mainly for MYC-driven disease research[1].

Product Specifications

CAS Number

[2407433-00-3]

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Apoptosis; CDK; DYRK

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/T025.html

Purity

99.64

Solubility

DMSO : 8.25 mg/mL (ultrasonic)

Smiles

CNC1=NC(NCC2=NC=CC=N2)=C(C(C3=CC=C(N=CC=C4)C4=C3)=CN5)C5=N1

Molecular Formula

C21H18N8

Molecular Weight

382.42

Precautions

H302, H315, H319

References & Citations

[1]Iwai K, et al. Anti-tumor efficacy of a novel CLK inhibitor via targeting RNA splicing and MYC-dependent vulnerability. EMBO Mol Med. 2018 Jun;10 (6) :e8289.