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616463

Sigma-Aldrich

TGF-β RI Kinase Inhibitor IX

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Synonym(s):
TGF-β RI Kinase Inhibitor IX, 4-((4-((2,6-Dimethylpyridin-3-yl)oxy)pyridin-2-yl)amino)benzenesulfonamide, ALK5 Inhibitor IX
Empirical Formula (Hill Notation):
C18H18N4O3S
Molecular Weight:
370.43

Assay

≥95% (HPLC)

Quality Level

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

2-8°C

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This Item
616454526528616452
form

powder

form

solid

form

powder

form

solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

storage condition

OK to freeze, protect from light

color

off-white

color

pale yellow

color

off-white

color

yellow

solubility

DMSO: 100 mg/mL

solubility

DMSO: 20 mg/mL

solubility

DMSO: 100 mg/mL, clear, nearly colorless, water: 100 mg/mL, clear, nearly colorless

solubility

DMSO: 5 mg/mL, methanol: 5 mg/mL

General description

A cell-permeable pyridinyloxypyridine compound that acts as a potent and highly selective inhibitor against TGFβ RI/ALK5 (IC50 = 72 nM, [ATP] = 1 mM) by targeting both the ATP-binding site and the “selectivity pocket”, while exhibiting much reduced or little activity against a panel of 75 other kinases (IC50<1 µM). Shown to reduce TGFβ1-induced nuclear translocation of a GFP-Smad2 fusion reporter in MDA-MB-468 cells (IC50 = 22 nM) in vitro and exhibit excellent oral bioavailability (F = 75%, AUC = 4.95 µM.h) with low clearance (12 ml/min/kg) in rats in vivo.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstiution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Goldberg, F.W., et al. 2009. J. Med. Chem.52, 7901.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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