R-268712

SKU: orb1307817

Description

R-268712 is a potent and orally bioavailable inhibitor of the TGF-β type I receptor/ALK5, exhibiting an IC50 of 2.5 nM. This small molecule is a valuable research tool for investigating TGF-β signaling in fibrosis, oncology, and immunology research, applicable in both cellular and animal models.

Research Area

Cardiovascular Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 879487-87-3
• MW: 363.39
• Purity: 99.77%
• Formula: C₂₀H₁₈FN₅O
• SMILES: Cc1cccc(n1)-c1n[nH]cc1-c1ccc(F)c(c1)-c1cnn(CCO)c1
• Target: ALK,TGF-beta/Smad
• Solubility: DMSO:250 mg/mL (687.97 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (11.01 mM)

Bioactivity

• Target IC50:
  TGFBR1:2.5 nM|Smad3:10.4 nM
• In Vivo:
  Oral administration of R-268712 at doses of 1, 3 and 10mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model. Additionally, the efficacy of R-268712 in a heminephrectomized anti-Thy1 glomerulonephritis model at doses of 0.3 and 1mg/kg. R-268712 reduced proteinuria and glomerulosclerosis significantly with improvement of renal function.
• In Vitro:
  R-268712 is a novel and specific inhibitor of activin receptor-like kinase 5 (ALK5), a transforming growth factor β (TGF-β) type I receptor. Evaluation of in vitro inhibition indicated that R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

renal fibrosis, TGFb, TGF-b/Smad, TGFβ, TGF-β, TGF-β/Smad, TGF-β Receptor, TGFbeta, TGF-beta, TGF-beta/Smad, TGFbeta/Smad, Smad, R 268712, Thy1 nephritis, R268712, R-268712, Transforming growth factor beta, Transforming growth factor beta receptors, UUO, inhibit, Inhibitor, HFL-1, glomerulonephritis, glomerulosclerosis, Anaplastic lymphoma kinase, Anaplastic lymphoma kinase (ALK), ALK5, ALK tyrosine kinase receptor, CKD, Cluster of differentiation 246, CD246

Compound Identifiers

PubChem CID

11703284