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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
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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Purity 99.27%

HNMR LCMS COA Datasheet MSDS

Purity 98.00%

HNMR COA Datasheet MSDS

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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Answers to questions you may have can be found in the Inhibitor Handling Instructions. Topics include how to prepare stock solutions, how to store Products, and issues that need special attention for cell-based assays and animal experiments.

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