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7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-(3S)-3-piperidinyl-2H-pyrido[2,3-d][1,3]oxazin-2-one

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7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-(3S)-3-piperidinyl-2H-pyrido[2,3-d][1,3]oxazin-2-one manufacturers
7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-(3S)-3-piperidinyl-2H-pyrido[2,3-d][1,3]oxazin-2-one Basic information
Product Name:7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-(3S)-3-piperidinyl-2H-pyrido[2,3-d][1,3]oxazin-2-one
Synonyms:7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-(3S)-3-piperidinyl-2H-pyrido[2,3-d][1,3]oxazin-2-one;Bay 65-1942 (free base);Bay 65-1942;2H-Pyrido[2,3-d][1,3]oxazin-2-one, 7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-(3S)-3-piperidinyl-;Bay 65 1942 free base,Bay 651942 free base
CAS:600734-02-9
MF:C22H25N3O4
MW:395.45
EINECS:
Product Categories:
Mol File:600734-02-9.mol
7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-(3S)-3-piperidinyl-2H-pyrido[2,3-d][1,3]oxazin-2-one Structure
7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-(3S)-3-piperidinyl-2H-pyrido[2,3-d][1,3]oxazin-2-one Chemical Properties
Boiling point 521.8±50.0 °C(Predicted)
density 1.286
storage temp. Store at -20°C
solubility Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
form Powder
pka8.07±0.35(Predicted)
Safety Information
MSDS Information
7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-(3S)-3-piperidinyl-2H-pyrido[2,3-d][1,3]oxazin-2-one Usage And Synthesis
UsesBay 65-1942 free base is an ATP-competitive and selective IKKβ inhibitor.
in vivo

Inhibitors of MEK (AZD6244) and IKK (BAY 65-1942) are used at their IC50 concentrations, as determined by a 48 hour MTS assay, which achieve sufficient inhibition of kinase activity. MYL-R cells are treated for 24 hours with AZD6244 (5 μM), BAY 65-1942 (10 μM), or a combination of these inhibitors at the same concentrations. AZD6244 and BAY 65-1942 demonstrate synergistic inhibition of cell viability at the dose combination (5 μM AZD6244+10 μM BAY 65-1942), which correlates with IC75 (CI=0.48±0.01). Synergism is also indicated at the IC50 (CI=0.56±0.09) and IC90 (CI=0.46±0.02) dose combinations reported by the software (CI values are the mean of three independent experiments, ± standard deviation). AZD6244 and BAY 65-1942 treatment induces 2- and 1.3-fold caspase 3/7 activation, respectively, compared to the DMSO-treated cells. Treatment with a combination of AZD6244 plus BAY 65-1942 leads to a 3.2-fold increase in caspase 3/7 activity[2].

IC 50IKKβ
References[1] Moss NC, et al. IKKbeta inhibition attenuates myocardial injury and dysfunction following acute ischemia-reperfusion injury. Am J Physiol Heart Circ Physiol. 2007 Oct;293(4):H2248-53. DOI:10.1152/ajpheart.00776.2007
[2] Cooper MJ, et al. Application of multiplexed kinase inhibitor beads to study kinome adaptations in drug-resistant leukemia. PLoS One. 2013 Jun 24;8(6):e66755. DOI:10.1371/journal.pone.0066755
7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-(3S)-3-piperidinyl-2H-pyrido[2,3-d][1,3]oxazin-2-one Preparation Products And Raw materials
Tag:7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-(3S)-3-piperidinyl-2H-pyrido[2,3-d][1,3]oxazin-2-one(600734-02-9) Related Product Information
7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride 2H-Pyrido[2,3-d][1,3]oxazin-2-one, 7-[2-(cyclopropylMethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-(4-piperidinyl)- (hydrochloride)(1:1) 1-Piperidinecarboxylic acid, 4-[7-[2-(cyclopropylmethoxy)-6-[(4-methoxyphenyl)methoxy]phenyl]-1,4-dihydro-2-oxo-2H-pyrido[2,3-d][1,3]oxazin-5-yl]-, 1,1-dimethylethyl ester 3-{7-[5-Bromo-2-(4-methoxybenzyloxy)-phenyl]-2-oxo-1,4-dihydro-2H-pyrido[2,3-d][1,3]oxazin-5-yl}-piperidine-1-carboxylic acid tert-butyl ester 1-Piperidinecarboxylic acid, 3-[7-[2-(cyclopropylmethoxy)-6-[(4-methoxyphenyl)methoxy]phenyl]-1,4-dihydro-2-oxo-2H-pyrido[2,3-d][1,3]oxazin-5-yl]-, 1,1-dimethylethyl ester 3-Pyridinecarboxylic acid, 2-amino-6-[2-(cyclopropylmethoxy)-6-[(4-methoxyphenyl)methoxy]phenyl]-4-[1-[(1,1-dimethylethoxy)carbonyl]-3-piperidinyl]-, 1,1-dimethylethyl ester