MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel-
- Product Name
- MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel-
- CAS No.
- 1254036-66-2
- Chemical Name
- MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel-
- Synonyms
- CS-2341;GSK2292767;PI3Kδ inhibitor GS2292767;PI3Kδ inhibitor GS2292767;rel-N-[5-[4-[5-[[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-methoxy-3-pyridinyl]methanesulfonamide;N-{5-[4-(5-{[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl}-1,3-oxazo l-2-yl)-1H-indazol-6-yl]-2-methoxy-3-pyridinyl}methanesulfonamide;MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel-;N-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1H-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methanesulfonamide
- CBNumber
- CB52628081
- Molecular Formula
- C24H28N6O5S
- Formula Weight
- 512.58
- MOL File
- 1254036-66-2.mol
MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- Property
- Melting point:
- 199-202°C
- Boiling point:
- 730.4±70.0 °C(Predicted)
- Density
- 1.360±0.06 g/cm3(Predicted)
- storage temp.
- -20°C Freezer, Under inert atmosphere
- solubility
- DMSO (Slightly), Methanol (Slightly)
- form
- Solid
- pka
- 6.29±0.50(Predicted)
- color
- White to Off-White
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 21757
- Product name
- GSK2292767
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 21757
- Product name
- GSK2292767
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $202
- Updated
- 2024/03/01
- Product number
- 21757
- Product name
- GSK2292767
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $363
- Updated
- 2024/03/01
- Product number
- 21757
- Product name
- GSK2292767
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $796
- Updated
- 2024/03/01
- Product number
- G797430
- Product name
- rel-N-[5-[4-[5-[[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-methoxy-3-pyridinyl]methanesulfonamide
- Packaging
- 1mg
- Price
- $45
- Updated
- 2021/12/16
MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- Chemical Properties,Usage,Production
Uses
rel-N-[5-[4-[5-[[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-methoxy-3-pyridinyl]methanesulfonamide is a selective PI3Kδ inhibitor for the treatment of respiratory disease (1,2).
Biological Activity
pki: 10.1gsk2292767 is a potent and selective pi3kδ inhibitor.phosphoinositide 3-kinase δ (pi3kδ), a lipid kinase belonging to the class 1 pi3k family with the closely homologous isoforms α and β, catalyzes the phosphorylation of phosphatidylinositol 4,5-bisphosphate, triggering various downstream biological events suvch as cell growth, proliferation, differentiation, and survival.
in vitro
gsk2292767 was found to be greater than 100-fold selective against a panel of in-house kinases and in the millipore panel. moreover, gsk2292767 could inhibit both ifnγ and il-2 production in a concentration-dependent manner in a human lung parenchyma assay, with pic50s of 8.7 and 8.5, respectively [1].
in vivo
in a rat pk study, the in vivo clearance for gsk2292767 was significantly higher than that for its analog gsk2269557. the oral bioavailability was also low (f < 2%), which was consistent with the data observed for gsk2269557. in a rabbit cardiac ventricular wedge assay, no effect on qt interval, tpe, or qrs and no significant risk of tdp arrhythmias was observed for gsk2292767 over the concentration range tested, thus indicating gsk2292767 could successfully mitigate the risk associated with gsk2269557. moreover, gsk2292767 was found to protect against eosinophil recruitment with an ed50 of 35 μg/kg in the brown norway rat acute ova model, which was similar to gsk2269557 [1].
References
[1] down k et al. optimization of novel indazoles as highly potent and selective inhibitors of phosphoinositide 3-kinase δ for the treatment of respiratory disease. j med chem. 2015 sep 24;58(18):7381-99.
MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- Preparation Products And Raw materials
Raw materials
Preparation Products
MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- Suppliers
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View Lastest Price from MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- manufacturers
- Product
- N-{5-[4-(5-{[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl}-1,3-oxazo l-2-yl)-1H-indazol-6-yl]-2-methoxy-3-pyridinyl}methanesulfonamide 1254036-66-2
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- Min98% HPLC
- Supply Ability
- g/kg/ton
- Release date
- 2019-12-20