7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide
- Product Name
- 7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide
- CAS No.
- 142557-61-7
- Chemical Name
- 7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide
- Synonyms
- A 484954;A-484954(A 484954);A-484954, 10 mM in DMSO;eEF2K Inhibitor, A-484954;eEF2K Inhibitor, A-484954 - CAS 142557-61-7 - Calbiochem;7-AMino-1-cyclopropyl-3-ethyl-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide;7-amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1H,2H,3H,4H-pyrido[2,3-d]pyrimidine-6-carboxamide;7-Amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-6-carboxamid;7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide;7-Amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-6-carboxamide
- CBNumber
- CB02621577
- Molecular Formula
- C13H15N5O3
- Formula Weight
- 289.29
- MOL File
- 142557-61-7.mol
7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide Property
- Boiling point:
- 522.9±60.0 °C(Predicted)
- Density
- 1.522±0.06 g/cm3 (20 ºC 760 Torr)
- storage temp.
- 2-8°C
- solubility
- DMSO: soluble3mg/mL, clear (warmed)
- pka
- 14.26±0.20(Predicted)
- form
- powder
- color
- white to beige
Safety
- Hazard Codes
- T
- Risk Statements
- 25-36/37/38
- Safety Statements
- 26-45
- RIDADR
- UN 2811 6.1 / PGIII
- WGK Germany
- 3
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H301Toxic if swalloed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 324516
- Product name
- eEF2K Inhibitor, A-484954
- Packaging
- 10mg
- Price
- $279
- Updated
- 2025/07/31
- Product number
- SML0861
- Product name
- A-484954
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $121
- Updated
- 2022/05/15
- Product number
- 28279
- Product name
- A-484954
- Packaging
- 5mg
- Price
- $116
- Updated
- 2024/03/01
- Product number
- 28279
- Product name
- A-484954
- Packaging
- 25mg
- Price
- $420
- Updated
- 2024/03/01
- Product number
- 28279
- Product name
- A-484954
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide Chemical Properties,Usage,Production
Description
A-484954 is an ATP-competitive inhibitor of eukaryotic elongation factor-2 kinase (eEF-2K; IC50 = 420 nM). It reduces eEF-2K autophosphorylation in PC3, HeLa, H460, H1299, and MDA-MB-231 cancer cells when used at a concentration of 75 μM.
Uses
A-484954 has been used a selective and potent inhibitor to inhibit eEF2K (eukaryotic elongation factor 2 kinase), in order to check the enhancement of synaptic transmission in the stratum radiatum of the hippocampal CA1 region. It has also been used as an eEF2K inhibitor to monitor real-time luminescence of U2OS Arntl::dLUC cells.
Uses
7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide,a pyrido[2,3-d]pyrimidin-2,4(1H,3H)-dione derivative with potential use as herbicide antidote.
Biochem/physiol Actions
A-484954 is a potent, selective inhibitor of eukaryotic longation factor-2 kinase (eEF2K). Eukaryotic elongation factor-2, which is required for protein synthesis, is inactivated upon phosphorylation by eEF2K.
in vivo
A484954 causes relaxation in E (+) and E (-) aorta or mesenteric artery precontracted with NA. Pretreatment with L-NAME but not indomethacin or cimetidine partially inhibits the A484954-induced relaxation in mesenteric artery[2].
Long-term A-484954 treatment inhibits MCT-induced increases PA pressure. It is revealed that A-484954 inhibits MCT-induced PA hypertrophy and fibrosis but not impairment of endothelium-dependent and -independent relaxation. Furthermore, A-484954 inhibits MCT-induced NADPH oxidase-1 expression and ROS generation as well as matrix metalloproteinase-2 activation[3].
storage
Store at +4°C
References
[1] RAMAKRISHNA EDUPUGANTI . Synthesis and biological evaluation of pyrido[2,3-d]pyrimidine-2,4-dione derivatives as eEF-2K inhibitors[J]. Bioorganic & Medicinal Chemistry, 2014, 22 17: Pages 4910-4916. DOI: 10.1016/j.bmc.2014.06.050
7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from 7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide manufacturers
- Product
- 7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide 142557-61-7
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 99.0%
- Supply Ability
- 100kg
- Release date
- 2020-01-18