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TAK-632

Catalog No. T1886 CAS 1228591-30-7

TAK-632 is a potent pan-Raf inhibitor.

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TAK-632, CAS 1228591-30-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 35.00
10 mg	In stock	$ 45.00
25 mg	In stock	$ 78.00
50 mg	In stock	$ 126.00
100 mg	In stock	$ 223.00
200 mg	In stock	$ 289.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.27%

Purity: 98.5%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	TAK-632 is a potent pan-Raf inhibitor.
Targets&IC50	PDGFRβ:120 nM, Aurora B:66 nM, FGFR3:280 nM, B-Raf:8.3 nM, C-Raf:1.4 nM
In vitro	In an SK-MEL-2 xenograft mouse model bearing NRAS-mutant melanoma, oral administration of TAK-632 (at doses of 60 or 120 mg/kg) inhibits the MAPK signaling pathway, thereby suppressing tumor growth.
In vivo	TAK-632 effectively inhibits cell proliferation in A375 (GI50=66 nM) and HMVII cell lines (GI50=200 nM). Specifically, in the melanoma A375 cell line (BRAFV600E), TAK-632 suppresses MEK phosphorylation (IC50=2 nM) and ERK phosphorylation (IC50=16 nM). Additionally, in the human melanoma HMVII cell line (NRASQ61K/BRAFG469V), TAK-632 inhibits pMEK (IC50=49 nM) and pERK (IC50=50 nM).
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)

Molecular Weight	554.52
Formula	C27H18F4N4O3S
CAS No.	1228591-30-7

Storage

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

Solubility Information

DMSO: 93 mg/mL (167.7 mM)

Ethanol: 2 mg/mL (3.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

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. 3. Zhang H, Xu L, Qin X, et al. N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl) phenyl) acetamido) phenoxy) benzo [d] thiazol-2-yl) cyclopropanecarboxamide (TAK-632) Analogues as Novel Necroptosis Inhibitors by Targeting Receptor-Interacting Protein Kinase 3 (RIPK3): Synthesis, Structure-Activity Relationships and In Vivo Efficacy[J]. Journal of Medicinal Chemistry. 2019 May 28.

Citations

1. Zhang H, Xu L, Qin X, et al. N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl) phenyl) acetamido) phenoxy) benzo [d] thiazol-2-yl) cyclopropanecarboxamide (TAK-632) Analogues as Novel Necroptosis Inhibitors by Targeting Receptor-Interacting Protein Kinase 3 (RIPK3): Synthesis, Structure-Activity Relationships and In Vivo Efficacy. Journal of Medicinal Chemistry. 2019 May 28

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Breast Cancer Compound Library Anti-Cancer Compound Library Osteogenesis Compound Library MAPK Inhibitor Library Bioactive Compound Library Anti-Fibrosis Compound Library

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GDC-0879 ARS-853 Cyclorasin 9A5 BMS-214662 RAF709 Pelitinib KRPEP-2D acetate Plx-4032

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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

TAK-632 1228591-30-7 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic MAPK Tyrosine Kinase/Adaptors Raf FGFR PDGFR Aurora Kinase inhibit Inhibitor TAK632 Raf kinases TAK 632 inhibitor

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