Narazaciclib

• Description :

  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 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2

• Isoform :

  CDK4; CDK6; NUAK1

• CAS Number :

  [1357470-29-1]