(1E) -CFI-400437 (dihydrochloride)

(1E) -CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM) . (1E) -CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity[1].

Product Specifications

CAS Number

[1247000-76-5]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Polo-like Kinase (PLK)

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/1e-cfi-400437-dihydrochloride.html

Purity

98.08

Solubility

DMSO : 12.5 mg/mL (ultrasonic) |H2O : 1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

Cl[H].Cl[H].COC1=CC(/C2=C/C3=CC4=C(C(/C=C/C5=CC=C(N=C5)N6CCN(CC6)C)=NN4)C=C3)=C(C=C1)NC2=O

Molecular Formula

C29H30Cl2N6O2

Molecular Weight

565.49

Precautions

H302, H315, H319, H335

References & Citations

[1]Laufer R, et al. The discovery of PLK4 inhibitors: (E) -3- ((1H-Indazol-6-yl) methylene) indolin-2-ones as novel antiproliferative agents. J Med Chem. 2013;56 (15) :6069-6087.