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.
Product information
CAS Number: 1976038-41-1
Molecular Weight: 411.82
Formula: C20H15ClFN5O2
Chemical Name: 2-{1-[2-(5-chloro-2-fluorophenyl)-5-methylpyridin-4-yl]-2-oxo-1H,2H,3H-imidazo[4,5-c]pyridin-3-yl}acetamide
Smiles: CC1=CN=C(C=C1N1C2C=CN=CC=2N(CC(N)=O)C1=O)C1=CC(Cl)=CC=C1F
InChiKey: LVEUPFUJRKZPEN-UHFFFAOYSA-N
InChi: InChI=1S/C20H15ClFN5O2/c1-11-8-25-15(13-6-12(21)2-3-14(13)22)7-17(11)27-16-4-5-24-9-18(16)26(20(27)29)10-19(23)28/h2-9H,10H2,1H3,(H2,23,28)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
References:
- Wang H, et al. Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors.Bioorg Med Chem Lett. 2016 Sep 1;26(17):4334-9.
Products are for research use only. Not for human use.
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