2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride

2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine  hydrate  hydrochloride
  • CAS No.:694433-59-5

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  1. This product is a chemical product/pharmaceutical intermediate. It is not a drug, an active pharmaceutical ingredient (API), or a pharmaceutical-grade material. It has not been granted a drug approval number or a Chemical Drug Substance Approval Notice, has not passed drug-related review and approval, and is not manufactured, tested, or released in accordance with pharmaceutical GMP.
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2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride Basic information
Product Name:2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride
Synonyms:2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride;SB-505124 hydrate hydrochloride;2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-iMidazol-4-yl)-6-Methylpyridine;2-[4-(1,3-Benzodioxol-5-yl)-2-(1,1- diMethylethyl)-1H-iMidazol-5-yl]-6-Methyl-pyridine;2-[4-(1,3-Benzodioxol-5-yl)-2-(tert-butyl)-1H-imidazol-5-yl]-6-methylpyridine;SB-505124, 98%, a selective inhibitor of TGFβR for ALK4, ALK5;SB-505124 hydrochloride hydrate;2-(4-(benzo[d][1,3]dioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl)-6-methylpyridine
CAS:694433-59-5
MF:C20H21N3O2
MW:335.4
EINECS:
Product Categories:Inhibitors;Smad;Aromatics;Heterocycles;Intermediates & Fine Chemicals;TGF-beta;Pharmaceuticals;Tyrosine Kinase Inhibitors
Mol File:694433-59-5.mol
2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride Chemical Properties
Melting point 168 °C
Boiling point 509.7±50.0 °C(Predicted)
density 1.202
storage temp. Sealed in dry,2-8°C
solubility DMSO: >10mg/mL
form powder
pka11.26±0.10(Predicted)
color yellow
Safety Information
Hazard Codes Xi
Risk Statements 36/37/38
Safety Statements 26-36
WGK Germany 3
HS Code 29349990
MSDS Information
2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride Usage And Synthesis
DescriptionSB-505124 inhibits the TGF-β1 receptor serine/threonine kinase ALK5 with an IC50 value of 47 nM. Though it is a less potent antagonist of ALK4 (IC50 = 129 nM) and ALK7, SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK7-dependent activation of downstream SMAD2 and SMAD3 and TGF-β–induced MAP kinase pathway components without altering ALK1-3 or ALK6-induced SMAD signaling. In an assay determining in vitro phosphorylation of SMAD3, SB-505124 is more potent than SB-431452 with IC50 values of 47 versus 94 nM, respectively.
UsesSB-505124 is a selective inhibitor of transforming growth factor-beta type I receptor ALK5 and as well as being a selective inhibitor of ALK4 but with less potency. SB-505124 blocks TGF-β–induced apoptosis of FaO cells and NRP 154 cells in a concentration-dependent manner. SB-505124 has been shown to suppress the migration and invasion of breast cancer MCF-7-M5 cells.
UsesSB-505124 inhibits the TGF-β1 receptor serine/threonine kinase ALK5 with an IC50 value of 47 nM. Though it is a less potent antagonist of ALK4 (IC50 = 129 nM) and ALK7, SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK7-dependent activation of downstream SMAD2 and SMAD3 and TGF-β–induced MAP kinase pathway components without altering ALK1-3 or ALK6-induced SMAD signaling. In an assay determining in vitro phosphorylation of SMAD3, SB-505124 is more potent than SB-431452 with IC50 values of 47 versus 94 nM, respectively.
UsesSB-505124 hydrochloride hydrate was used to study the role of TGF-β pathway in development and differentiation studies.3,4
Biochem/physiol ActionsSB-505124 selectively inhibits TGF-β type I receptors, activin receptor-like kinases (ALK) 4, 5 and 7. It inhibits ALK4-, 5- and 7-mediated activation of Smad2, Smad3 and MAPK pathway induced by TGF-β.1 SB-505124 inhibits the human fibroblast trans-differentiation induced by the co-culture with Esophageal squamous cell carcinoma.2
2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride Preparation Products And Raw materials

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