GZD856 (formic)

• Description:

  GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-AblT315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity[1][2]. GZD856 (formic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

• UNSPSC:

  12352005

• Target:

  Apoptosis; Bcr-Abl; PDGFR

• Type:

  Reference compound

• Related Pathways:

  Apoptosis; Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/gzd856-formic.html

• Purity:

  95.36

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  O=C(NC1=CC=C(CN2CCN(C)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(C#CC4=CN5C(N=C4)=CC=N5)=C3.OC=O

• Molecular Formula:

  C30H29F3N6O3

• Molecular Weight:

  578.58

• References & Citations:

  [1]Zhang Z, et, al. GZD856, a novel potent PDGFRα/β inhibitor, suppresses the growth and migration of lung cancer cells in vitro and in vivo. Cancer Lett. 2016 May 28;375 (1) :172-178.|[2]Lu X, et, al. Synthesis and identification of GZD856 as an orally bioavailable Bcr-Abl T315I inhibitor overcoming acquired imatinib resistance. J Enzyme Inhib Med Chem. 2017 Dec;32 (1) :331-336.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C (Powder, sealed storage, away from moisture)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  Bcr-Abl; PDGFRα; PDGFRβ

• CAS Number:

  [2804039-78-7]