1. TGF-beta/Smad
    Stem Cell/Wnt
    Protein Tyrosine Kinase/RTK
  2. TGF-β Receptor
    TGF-beta/Smad
    Anaplastic lymphoma kinase (ALK)
  3. R-268712

R-268712 

Cat. No.: HY-12953 Purity: 99.78%
Handling Instructions

R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer.

For research use only. We do not sell to patients.

R-268712 Chemical Structure

R-268712 Chemical Structure

CAS No. : 879487-87-3

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Solution
10 mM * 1 mL in DMSO USD 185 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 185 In-stock
Estimated Time of Arrival: December 31
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5 mg USD 168 In-stock
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10 mg USD 252 In-stock
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50 mg USD 1020 In-stock
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100 mg USD 1860 In-stock
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Description

R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer[1][2].

IC50 & Target

TGFBR1

2.5 nM (IC50)

Smad3

10.4 nM (IC50)

In Vitro

R-268712 (3, 10, 30, 100, 300 nM; 1 h) inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM in HFL-1 cells[1]. R-268712 (3, 10, 30, 100, 300 nM; 72 h) inhibits myofibroblast transdifferentiation (MTD) from fibroblasts in a dose-dependent manner without inhibition of cell growth in HFL-1cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HFL-1 cells
Concentration: 3, 10, 30, 100, 300 nM
Incubation Time: 1 or 72 h
Result: Inhibited the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM when incubation 1 h.
Suppressed myofibroblast transdifferentiation (MTD) from fibroblasts in a dose-dependent manner without inhibition of cell growth when incubation after 72 h.
In Vivo

R-268712 (0.3, 1, 3, 10 mg/kg; p.o.; single) shows AUC0-24 values of 0.075, 0.28, 1.6 and 8.2 μg•h/mL for dosages of 0.3, 1, 3, 10 mg/kg, respectively[2].
R-268712 (1, 3, 10 mg/kg; p.o.; single daily for 3 days) inhibits renal luciferase activity in a dose-dependent manner in UUO model[2].
R-268712 (0.3, 1 mg/kg; p.o.; single daily for 33 days) shows renoprotective effects (improves and maintains renal function as well as inhibits glomerular sclerosis) on Thy1 nephritis model when at dosage of 1 mg/kg[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male WKY/Hos rats[2].
Dosage: 0.3, 1, 3, and 10 mg/kg
Administration: Oral administration; single.
Result: 1.19 Pharmacokinetic Parameters of R-268712 in male WKY/Hos rats (n=4)[2].
PO (0.3 mg/kg) PO (1 mg/kg) PO (3 mg/kg) PO (10 mg/kg)
AUC0-24 (µg•h/mL) 0.075 0.28 1.6 8.2
Animal Model: Male Col1a1-Luc Tg rats (10 to14-week-old; UUO model; n=5-6)[2].
Dosage: 1, 3, 10 mg/kg
Administration: Oral administration; single daily for 3 days.
Result: Suppressed activity of renal luciferase in a dose-dependent manner.
Animal Model: Male WKY/Hos rats (4-week-old; Thy1 nephritis model; n=7)[2].
Dosage: 0.3, 1 mg/kg
Administration: Oral administration; single daily for 33 days.
Result: Significantly reduced proteinuria at day 21( the repression continued until day 28), and serum creatinine level (dosage at 1 mg/kg).
Apparently suppressed glomerular sclerosis by 28% and reduced the increase of the hydroxyproline content when at 1 mg/kg.
Suppressed the activation of mesangial parenchymal cell and the injury of podocyte on the basis of TGF-β signaling inhibition at 1 mg/kg.
Molecular Weight

363.39

Formula

C20H18FN5O

CAS No.
SMILES

FC1=C(C2=CN(CCO)N=C2)C=C(C3=CNN=C3C4=CC=CC(C)=N4)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (343.98 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7519 mL 13.7593 mL 27.5186 mL
5 mM 0.5504 mL 2.7519 mL 5.5037 mL
10 mM 0.2752 mL 1.3759 mL 2.7519 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.72 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.72 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.72 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.78%

References
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Product Name:
R-268712
Cat. No.:
HY-12953
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