1439934-41-4

Basic information

• Product Name: CTX0294885
• Synonyms: CTX0294885;2-(5-chloro-2-(4-(piperazin-1-yl)phenylaMino)pyriMidin-4-ylaMino)-N-MethylbenzaMide;2-(5-chloro-2-(4-(piperazin-1-yl)phenylamino)pyrimidin-4-ylamino)-N-methylbenzamide CTX0294885;CTX-0294885, >=98%;2-[[5-Chloro-2-[[4-(1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]-N-methylbenzamide
• CAS NO: 1439934-41-4
• Molecular Formula: C₂₂H₂₄ClN₇O
• Molecular Weight: 437.92526
• Product Categories: Inhibitors
• Mol File: 1439934-41-4.mol
• Article Data: 3

Chemical Properties

• Appearance: /
• Density: 1.332±0.06 g/cm3(Predicted)
• Solubility: ≥21.9 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
• PKA: 14.57±0.46(Predicted)
• CAS DataBase Reference: CTX0294885(CAS DataBase Reference)
• NIST Chemistry Reference: CTX0294885(1439934-41-4)
• EPA Substance Registry System: CTX0294885(1439934-41-4)

Safety Data

• Hazardous Substances Data: 1439934-41-4(Hazardous Substances Data)

Usage

Biological Activity

ctx-0294885 is a novel bisanilino pyrimidine. it has inhibitory activity towards a wild range of kinases in vitro. ctx-0294885 is capable of capturing more than half of the expressed kinome in mda-mb-231 cells. large-scale ctx-0294885-based affinity purification with lc?ms/ms identifies 235 protein kinases. ctx-0294885 binds additional kinases that were not identified from previous studies using other kinase capture reagents. it is further developed into a sepharose-supported kinase capture reagent. ctx-0294885 is a new tool for analysis of kinome signaling networks. [1]

references

1. zhang l, holmes ip, hochgr?fe f et al. characterization of the novel broad-spectrumkinase inhibitor ctx-0294885 as an affinity reagent for mass spectrometry-basedkinome profiling. j proteome res. 2013 jul 5;12(7):3104-16.

Upstream product

• 761440-08-8 2-[(2,5-dichloropyrimidin-4-yl)amino]-N-methyl-benzamide 
• 4141-08-6 2-Amino-N-methylbenzamid 
• 67455-41-8 4-(piperazin-1-yl)aniline 
• 1215504-60-1 4-(piperazin-1-yl)aniline hydrochloride 
• 118-48-9 isatoic anhydride 

Relevant articles and documents

Design, synthesis, and biological evaluation of novel covalent inhibitors targeting focal adhesion kinase

Forty-one new focal adhesion kinase (FAK) covalent inhibitors were designed and synthesized based on FAK inhibitor TAE226. Compound 11w displayed the highest inhibition of FAK with an IC50 value of 35 nM and exhibited potent anticancer activity against Hela, HCT116 and MDA-MB-231 cell lines with IC50 values of 0.41, 0.01 and 0.11 μM respectively, compared to TAE226 (2.68, 0.64 and 4.19 μM respectively). 11w also inhibited the clone formation and migration of HCT-116 cells and stimulated cell cycle arrest in the G2/M phase, inducing tumor cell apoptosis. Compound 11w formed a covalent bond with the Cys427 residue of FAK in a docking model, inhibiting the autophosphorylation of FAK and downstream proteins in a dose-dependent manner. Moreover, 11w showed adequate oral bioavailability of 21.02%. A 74.20% inhibition of tumor growth in the HCT116 xenograft model was also observed. These data indicate that 11w is a promising covalent inhibitor of FAK.

BINDING AGENT

The present disclosure generally relates to protein binding agents, such as protein kinase binding agents of general Formula (I). The protein binding agents may be provided attached to a solid support and may be used, for example, to detect the presence o