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Agerafenib

🥰Excellent
Catalog No. T2070Cas No. 1188910-76-0
Alias RXDX-105, CEP-32496, CEP32496, CEP 32496

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

Agerafenib

Agerafenib

🥰Excellent
Purity: 99.23%
Catalog No. T2070Alias RXDX-105, CEP-32496, CEP32496, CEP 32496Cas No. 1188910-76-0
Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.
Pack SizePriceAvailabilityQuantity
1 mg$35In Stock
5 mg$89In Stock
10 mg$133In Stock
25 mg$243In Stock
50 mg$397In Stock
100 mg$589In Stock
200 mg$842In Stock
1 mL x 10 mM (in DMSO)$97In Stock
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Purity:99.23%
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Product Introduction

Bioactivity
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)
In vitro
In the Colo-205 xenograft mouse model CEP-32496 (30 mg/kg, oral, BID) showed a 40% incidence of tumor arrest and partial tumor regression (PR), while the 100 mg/kg dose group showed an 80% incidence of tumor arrest and PR. Twice-daily oral treatment of tumor lysates with 30 mg/kg CEP-32496 inhibited 50% and 75% of normalized pMEK at 2 and 6 hours after dosing, respectively, whereas treatment of a mouse model bearing Colo-205 transplanted tumors with 55 mg/kg CEP-32496 for 2 to 10 hours inhibited 57% to 75% of pMEK. 32496 was orally bioavailable in a variety of preclinical species (> 95% in rats, dogs and monkeys).100 mg/kg CEP-32496 treatment resulted in inhibition of pMEK and pERK and sustained tumor arrest and regression in BRAF (V600E) colon cancer xenografts in nude mice.CEP-32496 showed good stability in mouse, dog, monkey, and human hepatic microsomal formulations. CEP-32496 exhibited good stability with intrinsic clearance values of <23 (μL/min)/ mg and t1/2> 60 min measured in all assays.
In vivo
CEP-32496 inhibited MAPK/MEK phosphorylation in human melanoma and colorectal cancer cell lines with IC50 of 78 nM and 60 nM.CEP-32496 inhibited the proliferation of A375 cells (BRAFV600E) with an EC50 of 78 nM.CEP-32496 acted on tumor cell lines, and inhibited the proliferation of A375, SK-MEL-28, CEP-32496 acts on tumor cell lines and is more sensitive to the cytotoxicity of mutant BRAF-expressing A375, SK, MEL-28, Colo-205, Colo-679 and HT-144 cells than wild-type BRAF-expressing HCT116, Hs578T, LNCaP, DU145 and PC-3 cells.
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)
AliasRXDX-105, CEP-32496, CEP32496, CEP 32496
Chemical Properties
Molecular Weight517.46
FormulaC24H22F3N5O5
Cas No.1188910-76-0
SmilesCOc1cc2ncnc(Oc3cccc(NC(=O)Nc4cc(on4)C(C)(C)C(F)(F)F)c3)c2cc1OC
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 45 mg/mL (86.96 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9325 mL9.6626 mL19.3252 mL96.6258 mL
5 mM0.3865 mL1.9325 mL3.8650 mL19.3252 mL
10 mM0.1933 mL0.9663 mL1.9325 mL9.6626 mL
20 mM0.0966 mL0.4831 mL0.9663 mL4.8313 mL
50 mM0.0387 mL0.1933 mL0.3865 mL1.9325 mL

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