1. TGF-beta/Smad
  2. TGF-β Receptor
  3. R-268712

R-268712 

Cat. No.: HY-12953 Purity: 99.70%
Handling Instructions

R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.

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

R-268712 Chemical Structure

R-268712 Chemical Structure

CAS No. : 879487-87-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 185 In-stock
Estimated Time of Arrival: December 31
5 mg USD 168 In-stock
Estimated Time of Arrival: December 31
10 mg USD 252 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1860 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM. IC50 value: 2.5 nM [1] Target: ALK5 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. R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). R-268712 is a weak inhibitor of p38 MAP kinase (IC50: 12.1 μM).[1] in vivo: Oral administration of R-268712 at doses of 1, 3 and 10 mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model. [1]

Molecular Weight

363.39

Formula

C₂₀H₁₈FN₅O

CAS No.

879487-87-3

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 provided by MCE.
References

Purity: 99.70%

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R-268712
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HY-12953
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