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GZD856 (formic)

$400$3,400

Products Details

Product 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.

Web ID

– HY-101489A

Storage Temperature

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

Shipping

– Blue Ice

Applications

– Cancer-Kinase/protease

Molecular Formula

– C30H29F3N6O3

References

– [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.

CAS Number

– 2804039-78-7

Molecular Weight

– 578.58

Compound Purity

– 98.06

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

Clinical Information

– No Development Reported

Research Area

– Cancer

Solubility

– DMSO : 100 mg/mL (ultrasonic)

Target

– Apoptosis;Bcr-Abl;PDGFR

Isoform

– Bcr-Abl;PDGFRα;PDGFRβ

Pathway

– Apoptosis;Protein Tyrosine Kinase/RTK

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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