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Agerafenib

Catalog No. T2070 CAS 1188910-76-0

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

CEP-32496 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

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	CEP-32496 is a highly potent inhibitor of BRAF.
Targets&IC50	PDGFRβ:2 nM(Kd), Lck:2 nM(Kd), Abl1:3 nM(Kd), c-Kit: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	CEP32496, CEP 32496, RXDX-105, CEP-32496
Molecular Weight	517.46
Formula	C24H22F3N5O5
CAS No.	1188910-76-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: <1 mg/mL

DMSO: 9 mg/mL (17.39 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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.

Dose Conversion

You can also refer to dose conversion for different animals. More

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
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The answer of 19.713 mg appears in the Mass box

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An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
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The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Tech Support

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 Src PDGFR c-Kit c-RET Bcr-Abl Raf RXDX 105 CEP32496 CEP 32496 RXDX-105 CEP-32496 RXDX105 Inhibitor Raf kinases inhibit inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.