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BIBF0775

Catalog No. T5197 CAS 334951-90-5

BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).

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BIBF0775, CAS 334951-90-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 60.00
5 mg	In stock	$ 147.00
10 mg	In stock	$ 228.00
25 mg	In stock	$ 378.00
50 mg	In stock	$ 531.00
100 mg	In stock	$ 768.00
500 mg	In stock	$ 1,580.00
1 mL * 10 mM (in DMSO)	In stock	$ 162.00

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Purity: 99.45%

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Description	BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).
Targets&IC50	ALK5:34 nM
Kinase Assay	The inhibition of the kinase activity of TGFβRI was determined using the Promega Kinase-Glo kit according to the manufacturer's protocol in the presence of 600 nM ATP. N-terminally his-tagged human TGFβRI (aa 162-end) expressed in baculovirus and purified using nickel affinity chromatography was used at a final concentration of 0.03 μg/mL. The inhibition of the kinase activity of PDGFRR was determined using the Z0-LYTE assay technology according to the manufacturer's protocol. Full-length human PDGFRR (5.6 nM per assay) and the Tyr4 peptide (2 μM per assay) were obtained from Invitrogen, too. IC50 values were determined by the use of the Graph PadPrism software.
Cell Research	The high-content cytotoxicity assay (kit I) was performed according to the manufacturer's instructions. HaCaT cells were cultured overnight in black 96-well plates, incubated for 24 h with each compound at different concentrations, and stained with cytotoxicity cocktail. Cells were fixed, washed, and scanned on the Cellomics ArrayScan II platform. Images were analyzed with the Cell Health image analysis algorithm. Cytotoxicity indices were calculated for each of the four parameters (cellular membrane integrity, nuclear fragmentation and density, and lysosomal mass) to indicate the percentage of cells outside of the normal range which was defined using a vehicle-treated reference cell population.

Molecular Weight	494.63
Formula	C31H34N4O2
CAS No.	334951-90-5

Storage

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

Solubility Information

DMSO: 60 mg/mL

References and Literature

1. Roth GJ, et al. Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factor β receptor I (TGFβRI). J Med Chem. 2010 Oct 28;53(20):7287-95.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library TGF-beta/Smad Compound Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Covalent Inhibitor Library Reprogramming Compound Library Stem Cell Differentiation Compound Library Anti-Lung Cancer Compound Library Anti-Breast Cancer Compound Library Anti-Fibrosis Compound Library

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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

BIBF0775 334951-90-5 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors TGF-beta/Smad ALK BIBF-0775 inhibit Transforming growth factor beta receptors TGF-β Receptor BIBF 0775 Inhibitor inhibitor

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