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Angiogenesis FGFR TAK632

TAK632

Catalog No. T1886   CAS 1228591-30-7
Purity 99.27% Datasheet

TAK-632 is a potent pan-Raf inhibitor.

TAK632, CAS 1228591-30-7
Pack Size Availability Price/USD Quantity
2 mg In stock 20.00
5 mg In stock 35.00
10 mg In stock 50.00
25 mg In stock 87.00
50 mg In stock 140.00
100 mg In stock 248.00
200 mg In stock 322.00
1 mL * 10 mM (in DMSO) In stock 50.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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Description TAK-632 is a potent pan-Raf inhibitor.
Targets&IC50 Aurora B :ic50 66nM,   B-Raf :ic50 8.3nM,   C-Raf :ic50 1.4nM,   FGFR3 :ic50 280nM,   PDGFRβ :ic50 120nM,  
Kinase Assay Kinase Profile Assay: Assays for serine/threonine kinases using radio labeled [γ-33P] ATP are performed in 96 well plates. BRAF and c-RAF are expressed as N-terminal FLAG-tagged protein using a baculovirus expression system. The reaction conditions are optimized for each kinase: BRAF (25 ng/well of enzyme, 1 μg/well of GST-MEK1(K96R), 0.1 μCi/well of [γ-32P] ATP, room temperature, 20 min reaction); c-RAF (25 ng/well of enzyme, 1 μg/well of GST-MEK1 (K96R), 0.1 μCi/well of [γ-32P] ATP, room temperature, 20 min reaction). Enzyme reactions are performed in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol and 0.5 μM ATP containing optimized concentration of enzyme, substrate and radiolabeled ATP as described above in a total volume of 50 μL. Prior to the kinase reaction, compound and enzyme are incubated for 5 min at reaction temperature as described above. The kinase reactions are initiated by adding ATP. After the reaction period as described above, the reactions are terminated by the addition of 10% (final concentration) trichloroacetic acid. The [γ-33P] or [γ-32P]-phosphorylated proteins are filtered in GFC filter plates with a Cell Harvester and then the plates are washed out with 3% phosphoric acid. The plates are dried, followed by the addition of 40 μL of MicroScint0. The radioactivity is counted by a TopCount scintillation counter.
Cell Research
The cells are proliferated in appropriate medium (vender recommended) supplemented with 10% heat-inactivated fetal bovine serum (FBS) and antibiotics, in tissue culture dishes placed in a humidified incubator maintained at 37°C in an atmosphere of 5% CO2 and 95% air. The anti-proliferative activity of compound is determined by treating cell lines with the compound for 3 days, followed by measurement of viable cell number in the Cell Titer-Glo assay. The cells are seeded in a 96-multiwell plate at 1500 to 4000 cells per well in medium containing FBS and cells allowed to sit down overnight. After 18–20 h, compounds at various concentrations by serial dilution are added to the cells and were cultured for 3 days in chamber. After the treatment culture, cellular proliferation is determined by a Cell Titer-Glo Luminescent Cell Viability Assay. In brief, 100 bL/well of Cell Titer-Glo Substrate solution is added to each well and the cells were cultured for an additional 10 minutes (approximately). The chemi-luminescence value is measured using a Luminescence Counter 1420 ARVO MX Light. Concentration response curves are generated by calculating the decrease in chemi-luminescence values in compound-treated samples relative to the vehicle (DMSO) treated controls. (Only for Reference)
Cell lines: A375 and HMVII cells
Animal Research
Animal Model: Human melanoma A375 (BRAFV600E) xenograft model and human melanoma HMVII (NRASQ61K/BRAFG469V) xenograft model in rats.
Molecular Weight 554.52
Formula C27H18F4N4O3S
CAS No. 1228591-30-7

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 93 mg/mL (167.7 mM)

Ethanol: 2 mg/mL (3.6 mM)

Water: <1 mg/mL

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

Solution 1

2% DMSO+98% PEG 300: 5 mg/mL

Citations

References and Literature
1. Okaniwa M, et al. J Med Chem. 2013, 56(16), 6478-6494. 2. Nakamura A, et al. Cancer Res. 2013, 73(23), 7043-7055.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Epigenetics Compound Library MAPK Inhibitor Library Tyrosine kinase inhibitor library DNA Damage & Repair Compound Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Fluorochemical Library Angiogenesis related Compound Library Preclinical Compound Library Cell cycle related Compound Library

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