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Agerafenib

Catalog No. T2070 CAS 1188910-76-0

Synonyms: RXDX-105, CEP 32496, CEP-32496, CEP32496

Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Agerafenib, CAS 1188910-76-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 133.00
25 mg	In stock	$ 243.00
50 mg	In stock	$ 397.00
100 mg	In stock	$ 593.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

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Purity: 99.23%

Purity: 95.78%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.
Targets&IC50	c-Kit:2 nM(Kd), PDGFRβ:2 nM(Kd), Abl-1:3 nM(Kd), Lck:2 nM(Kd), RET:2 nM(Kd)
Kinase Assay	Binding assay: Kinases are produced displayed on T7 phage or by expression in HEK-293 cells and tagged with DNA. Binding reactions are performed at room temperature for 1 hour, and the fraction of kinase not bound to test compound is determined by capture with an immobilized affinity ligand and quantitation by quantitative PCR. Each kinase is tested individually against CEP-32496. Kd values are determined using eleven serial 3-fold dilutions and presented as mean values from experiments performed in duplicate. Variability between individual values is less than 2-fold.
Cell Research	Cells are seeded at 104 cells per well in DMEM with 10% fetal calf serum and allowed to attach. The cells are washed with PBS and switched to DMEM with 0.5% of serum and incubated overnight. CEP-32496 is then added at various concentrations with a final DMSO concentration of 0.5% and incubated for 72 h. At the end of incubation, a Cell Titer Blue is added per instructions, and incubation is continued for 3 hours. Remaining viable cells are quantified by measuring the strength of the fluorescence signal using SoftMax Pro (excitation at 560 nm and emission at 590 nm). IC50 values are derived using a 9-point curve fitted with Igor Pro and are presented as mean values from experiments performed in duplicate. Variability between individual values is less than 2-fold.(Only for Reference)

Synonyms	RXDX-105, CEP 32496, CEP-32496, CEP32496
Molecular Weight	517.46
Formula	C24H22F3N5O5
CAS No.	1188910-76-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 9 mg/mL (17.39 mM)

References and Literature

1. Rowbottom MW, et al. J Med Chem, 2012, 55(3), 1082-1105. 2. James J, et al. Mol Cancer Ther, 2012, 11(4), 930-941.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library Autophagy Compound Library HIF-1 Signaling Pathway Compound Library

Related Products

Related compounds with same targets

Pseudoginsenoside Rh2 Lifirafenib Sorafenib tosylate PLX-4720 BAY-293 Griffipavixanthone CCT241161 RAF709

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Agerafenib 1188910-76-0 Angiogenesis Apoptosis Cytoskeletal Signaling MAPK Tyrosine Kinase/Adaptors Raf c-RET c-Kit Src Bcr-Abl PDGFR RXDX 105 RXDX-105 Inhibitor Raf kinases inhibit CEP 32496 CEP-32496 CEP32496 RXDX105 inhibitor

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