ChemicalBook > CAS DataBase List > 7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride

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

Product Name
7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride
CAS No.
600734-06-3
Chemical Name
7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride
Synonyms
Bay 65-1942 HCl;KINK-1 hydrochloride;Bay 65-1942 (HCl salt);Bay 65-1942 (hydrochloride);KINK-1 hydrochloride >=98% (HPLC);Bay 651942 hydrochloride,Bay 65 1942 hydrochloride;(S)-7-(2-(cyclopropylmethoxy)-6-hydroxyphenyl)-5-(piperidin-3-yl)-1H-pyrido[2,3-d][1,3]oxazin-2(4H)-one hydrochloride;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-[(3S)-3-piperidinyl]-,Hydrochloride(1:1)
CBNumber
CB02484912
Molecular Formula
C22H25N3O4.ClH
Formula Weight
431.917
MOL File
600734-06-3.mol
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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 hydrochloride Property

storage temp. 
-20°C
solubility 
DMSO : 50 mg/mL (115.76 mM; Need ultrasonic)
form 
powder
color 
white to beige
optical activity
[α]/D -19 to -24°, c = 0.2 in DMF
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2098
Product name
KINK-1 hydrochloride
Purity
≥98% (HPLC)
Packaging
5mg
Price
$190.8
Updated
2025/07/31
Sigma-Aldrich
Product number
SML2098
Product name
KINK-1 hydrochloride
Purity
≥98% (HPLC)
Packaging
25mg
Price
$676
Updated
2025/07/31
ChemScene
Product number
CS-0623
Product name
Bay65-1942hydrochloride
Purity
99.22%
Packaging
2mg
Price
$264
Updated
2021/12/16
ApexBio Technology
Product number
A3230
Product name
Bay65-1942HClsalt
Packaging
2mg
Price
$347
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
CCH0032208
Product name
7-[2-(CYCLOPROPYLMETHOXY)-6-HYDROXYPHENYL]-1,4-DIHYDRO-5-[(3S)-3-PIPERIDINYL]-2H-PYRIDO-[2,3-D][1,3]-OXAZIN-2-ONE HYDROCHLORIDE
Purity
95.00%
Packaging
2MG
Price
$414
Updated
2021/12/16
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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 hydrochloride Chemical Properties,Usage,Production

Uses

Bay 65-1942 hydrochloride is an ATP-competitive and selective IKKβ inhibitor.

Biochem/physiol Actions

KINK-1 (Kinase Inhibitor of NF-ΚB-1; Bay 65-1942; CmpdA; Compound A) is an ATP-competitive, IKKβ-selective IΚB kinase (IKK) inhibitor (Ki against ATP = 2 nM/IKKβ and 135 nM/IKKα) that potently inhibits IKKβ-catalyzed GST-IΚBα(1–54) phosphorylation (IC50 = 4 nM, 200 nM ATP) without affecting (IC50 >10μM) IKK3 or 27 other kinases, lipases, phosphatases, caspases, and MMPs. KINK-1 effectively inhibits NF-ΚB activation and cytokines production in various human and murine cultures (IC50 from 18 to 502 nM) and is efficacious against LPS-induced plasma TNF-α production in mice and rats in vivo (EC50 = 9.1 and 6.6 mg/kg p.o., repectively) with good pharmacokinetic profile and oral availability. KINK-1 is also shown to effectively inhibit OVA-induced lung inflammation in a rat model of asthma (ED50 <0.3 mg/kg p.o.) without adverse effects to the animals.

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 50

IKKβ

References

[1] Inhibition of IκB kinase-β protects dopamine neurons against lipopolysaccharide-induced neurotoxicity By Zhang, Feng; Qian, Li; Flood, Patrick M.; Shi, Jing-Shan; Hong, Jau-Shyong; Gao, Hui-Ming J Pharmacol Exp Ther. 2010 June; 333(3): 822-833. 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 hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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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 hydrochloride Suppliers

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600734-06-3, 7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride Related Search:

Avobenzone p-Anisidine

  • Bay 65-1942 (HCl salt)
  • Bay 65-1942 HCl
  • Bay 65-1942 (hydrochloride)
  • (S)-7-(2-(cyclopropylmethoxy)-6-hydroxyphenyl)-5-(piperidin-3-yl)-1H-pyrido[2,3-d][1,3]oxazin-2(4H)-one hydrochloride
  • 7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride
  • KINK-1 hydrochloride
  • KINK-1 hydrochloride >=98% (HPLC)
  • 2H-Pyrido[2,3-d][1,3]oxazin-2-one,7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-,Hydrochloride(1:1)
  • Bay 651942 hydrochloride,Bay 65 1942 hydrochloride
  • 600734-06-3
  • C22H25N3O4HCl