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R 268712

Cat. No. 5288 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Potent and selective inhibitor of TGF-βRI
Chemical Name: 4-[2-Fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-1H-pyrazole-1-ethanol
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (3)
Pathways (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for R 268712

R 268712 is a potent and selective inhibitor of the TGF-β type I receptor/ALK5 (IC50 = 2.5 nM). Exhibits ~5000-fold selectivity over p38 MAPK. Suppresses development of renal fibrosis in a unilateral ureteral obstruction model. Also reduces proteinuria, glomerulosclerosis and improves renal function in an anti-Thy1 glomerulonephritis model. Orally bioavailable.

Compound Libraries for R 268712

R 268712 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for R 268712

M. Wt 363.39
Formula C20H18FN5O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 879487-87-3
PubChem ID 11703284
InChI Key JQGOCCALXFSRHZ-UHFFFAOYSA-N
Smiles OCCN1N=CC(C2=C(F)C=CC(C3=CNN=C3C4=CC=CC(C)=N4)=C2)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for R 268712

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36.34 100
ethanol 18.17 50

Preparing Stock Solutions for R 268712

The following data is based on the product molecular weight 363.39. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.75 mL 13.76 mL 27.52 mL
5 mM 0.55 mL 2.75 mL 5.5 mL
10 mM 0.28 mL 1.38 mL 2.75 mL
50 mM 0.06 mL 0.28 mL 0.55 mL

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References for R 268712

References are publications that support the biological activity of the product.

Terashima et al (2014) R-268712, an orally active transforming growth factor-β type I receptor inhibitor, prevents glomerular sclerosis in a Thy1 nephritis model. Eur.J.Pharmacol. 734 60 PMID: 24726873

If you know of a relevant reference for R 268712, please let us know.

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Keywords: R 268712, R 268712 supplier, R268712, potent, selective, inhibitors, inhibits, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1, ALK5, ALK, receptors, activin, receptor-like, Kinases, transforming, growth, factor, β, kidney, TGF-beta, Receptors, 5288, Tocris Bioscience

Citations for R 268712

Citations are publications that use Tocris products.

Currently there are no citations for R 268712. Do you know of a great paper that uses R 268712 from Tocris? Please let us know.

Reviews for R 268712

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Literature in this Area

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Stem Cell Research Product Guide

Stem Cell Research Product Guide

This product guide provides a background to the use of small molecules in stem cell research and lists over 200 products for use in:

  • Self-renewal and Maintenance
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Stem Cells Scientific Review

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Stem Cells Poster

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.

Pathways for R 268712

TGF-β Signaling Pathway

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.