1. Protein Tyrosine Kinase/RTK
  2. ALK
  3. TGFβRI-IN-2

TGFβRI-IN-2 

Cat. No.: HY-125851
Handling Instructions

TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.

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

TGFβRI-IN-2 Chemical Structure

TGFβRI-IN-2 Chemical Structure

CAS No. : 1976038-41-1

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Description

TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose[1].

IC50 & Target

IC50: ALK 5[1]

In Vitro

TGFβRI-IN-2 (compound 18) at 1 μM shows a 31% inhibition of MAP3K2 (MEKK2) with an IC50 value of 2.2 μM[1].

In Vivo

TGFβRI-IN-2 (oral administation; 50, 150 and 500 mg/kg; 5 days) induces cardiovascular toxicity characterized by valvular interstitial cell proliferation, neutrophil presence, hemorrhage and fibrin deposition in the heart valves[1].

Animal Model: Rats[1]
Dosage: 50, 150 and 500 mg/kg
Administration: Oral administation; 50, 150 and 500 mg/kg; 5 days
Result: Induced cardiovalvulopathy in both the medium and high dose animal groups.
Molecular Weight

411.82

Formula

C₂₀H₁₅ClFN₅O₂

CAS No.

1976038-41-1

SMILES

O=C(N)CN(C1=C2C=CN=C1)C(N2C3=CC(C4=CC(Cl)=CC=C4F)=NC=C3C)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

TGFβRI-IN-2ALKAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246cardiovasculartoxicityInhibitorinhibitorinhibit

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TGFβRI-IN-2
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HY-125851
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