TGF-# RI KINASE INHIBITOR IX 1PC X 10MG

Code: 616463-10MG D2-231

General description

A cell-permeable pyridinyloxypyridine compound that acts as a potent and highly selective inhibitor against TGFβ RI/ALK5 (IC50 = 72 nM, [A...


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€289.02 EACH
Discontinued
€355.49 inc. VAT

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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)

assay≥95% (HPLC)
coloroff-white
formpowder
manufacturer/tradenameCalbiochem®
Quality Level100
shipped inambient
solubilityDMSO: 100 mg/mL
storage conditionprotect from light, OK to freeze
storage temp.2-8°C
Cas Number1117684-36-2
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