Narazaciclib

Narazaciclib (ON123300), a strong and brain-penetrant[1] multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM) . Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors[2]. Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM[3].

Product Specifications

CAS Number

[1357470-29-1]

Product Name Alternative

ON123300

UNSPSC

12352005

Hazard Statement

H302

Target

AMPK; CDK; PDGFR

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

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

Concentration

10mM

Purity

98.66

Solubility

DMSO : 16.67 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

N#CC1=CC2=CN=C(NC3=CC=C(N4CCN(C)CC4)C=C3)N=C2N(C5CCCC5)C1=O

Molecular Formula

C24H27N7O

Molecular Weight

429.52

Precautions

H302

References & Citations

[1]Hua Lv, et al. Integrated pharmacokinetic-driven approach to screen candidate anticancer drugs for brain tumor chemotherapy. AAPS J. 2013 Jan;15 (1) :250-7.|[2]Xiaoping Zhang, et al. Preclinical pharmacological evaluation of a novel multiple kinase inhibitor, ON123300, in brain tumor models. Mol Cancer Ther. 2014 May;13 (5) :1105-16.|[3]S K A Divakar, et al. Dual inhibition of CDK4/Rb and PI3K/AKT/mTOR pathways by ON123300 induces synthetic lethality in mantle cell lymphomas. Leukemia. 2016 Jan;30 (1) :86-93.