PhiKan-083 Hydrochloride
- Product Name
- PhiKan-083 Hydrochloride
- CAS No.
- 880813-36-5
- Chemical Name
- PhiKan-083 Hydrochloride
- Synonyms
- PK083;PhiKan 083;PhiKan-083 Hydrochloride;9-Ethyl-N-methyl-carbazole-3-methanamine;9H-Carbazole-3-methanamine, 9-ethyl-N-methyl-;[(9-Ethyl-9H-carbazol-3-yl)methyl](methyl)amine;9-Ethyl-N-methyl-9H-carbazole-3-methanamine hydrochloride;PhiKan 083,PhiKan-083,Inhibitor,MDM-2/p53,PhiKan083,inhibit
- CBNumber
- CB02652533
- Molecular Formula
- C16H18N2
- Formula Weight
- 238.33
- MOL File
- 880813-36-5.mol
PhiKan-083 Hydrochloride Property
- Boiling point:
- 401.0±27.0 °C(Predicted)
- Density
- 1.09±0.1 g/cm3(Predicted)
- storage temp.
- Store at 4°C
- solubility
- <13.74mg/ml in H2O; <27.48mg/ml in DMSO
- form
- solid
- pka
- 9.71±0.10(Predicted)
- color
- 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
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
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.
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.
P362Take off contaminated clothing and wash before reuse.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 4326
- Product name
- PhiKan083
- Purity
- ≥99%(HPLC)
- Packaging
- 10
- Price
- $199
- Updated
- 2021/12/16
- Product number
- 4326
- Product name
- PhiKan083
- Purity
- ≥99%(HPLC)
- Packaging
- 50
- Price
- $788
- Updated
- 2021/12/16
- Product number
- 256233
- Product name
- PhiKan 083
- Packaging
- 10mg
- Price
- $446
- Updated
- 2021/12/16
- Product number
- 1949CN
- Product name
- 1-(9-Ethyl-9H-carbazol-3-yl)-N-methylmethanamine
- Packaging
- 100mg
- Price
- $714
- Updated
- 2021/12/16
- Product number
- 1949CN
- Product name
- 1-(9-Ethyl-9H-carbazol-3-yl)-N-methylmethanamine
- Packaging
- 250mg
- Price
- $727
- Updated
- 2021/12/16
PhiKan-083 Hydrochloride Chemical Properties,Usage,Production
Uses
PhiKan-083 is a p53 stabilizing agent. PhiKan-083 preferentially binds mutated (Y220C) p53 over wild-type p53 at a site distinct from functional DNA/protein interaction regions. PhiKan-083 slows rate of thermal denaturation of p53-Y220C.
Biological Activity
ki: ≈ 150 mphikan 083 is a critical p53 stabilizing agent by bonding its mutation y220cthe mutation y220c of p53 exists a surface cavity that destabilizes the protein by 4 kcal/mol, at a site that is not functional. a p53 stabilizing agent binding it is able to slow rate of thermal denaturation [1].
in vitro
isothermal titration of phikan083 with t-p53c-y220c exhibited 1:1 stoichiometry and a kd of 125 ± 10 m. phikan083 stabilized t-p53c-y220c in a concentration-dependent manner. in a simple binding model for phikan083 (t-p53c-y220c at 310 k (37°c)), in the absence of ligand, the protein gave a half-life of 3.8 min, while it increased to 15.7 min at saturating concentrations of phikan083. this is a proposed anticancer drug that could be developed for the y220c mutant using p53 stabilizing agent. the site of mutation in the oncogenic y220c mutant phikan083 binds with reasonable affinity is a druggable target. interestingly, the site of mutation does not exist in a region of the protein that is functionally important, it will be an excellent target for drug stabilization therapy. this suggests the crystal structure of the complex will be a fresh start for further rounds of drug design and refinement [1].
References
[1] boeckler fm, joerger ac, jaggi g, rutherford tj, veprintsev db, fersht ar. targeted rescue of a destabilized mutant of p53 by an in silico screened drug. proc natl acad sci u s a. 2008 jul 29; 105(30):10360-5.
PhiKan-083 Hydrochloride Preparation Products And Raw materials
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