TAK-285

TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR (HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity[1]. TAK-285 can cross the blood-brain barrier (BBB) [2].

Product Specifications

CAS Number

[871026-44-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/TAK-285.html

Purity

98.99

Solubility

DMSO : ≥ 50 mg/mL

Smiles

ClC(C=C(NC1=NC=NC2=C1N(CCNC(CC(C)(C)O)=O)C=C2)C=C3)=C3OC4=CC=CC(C(F)(F)F)=C4

Molecular Formula

C26H25ClF3N5O3

Molecular Weight

547.96

Precautions

H302, H315, H319, H335

References & Citations

[1]Ishikawa T, et al. Design and synthesis of novel human epidermal growth factor receptor 2 (HER2) /epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold. J Med Chem. 2011 Dec 8;54 (23) :8030-50.|[2]Erdo F, et al. Verification of brain penetration of the unbound fraction of a novel HER2/EGFR dual kinase inhibitor (TAK-285) by microdialysis in rats. Brain Res Bull. 2012 Mar 10;87 (4-5) :413-9.