PD184352
Synonym(s):2-(2-Chloro-4-iodophenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide;CI-1040
- CAS NO.:212631-79-3
- Empirical Formula: C17H14ClF2IN2O2
- Molecular Weight: 478.66
- MDL number: MFCD02683961
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is PD184352?
Chemical properties
Off-White to Pale Beige Solid
The Uses of PD184352
An inhibitor of ERK signaling pathway. A MAP kinase inhibitor
The Uses of PD184352
An inhibitor of ERK signaling pathway. A MAP kinase inhibitor. Potent MEK inhibitor.
What are the applications of Application
PD 184,352 is a MEK inhibitor
Definition
ChEBI: 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide is an aminobenzoic acid.
Biological Activity
pd184352 (also known as ci-1040), a benzhydroxamate derivative, is a potent and highly selective mek1/2, two members of the family of mapkks, inhibitor that inhibits purified mek1 with ic50 of 17 nm in a non-atp and non-erk1/2 competitive manner [1].pd184352 binds to a hydrophobic pocket, which is located in a region with low sequence homology to other kinases, adjacent to the mg-atp binding site of mek1 and mek2 inducing a conformational change in un-phosphorylated mek1/2 and hence inactivating the un-phosphorylated mek1/2 [1].pd184352 has been found to be actively against tumors, where it inhibits the growth of colon carcinomas in mouse xenograft models [1].
Biochem/physiol Actions
PD184352 (CI-1040) is a highly selective non-competitive inhibitor of MEK (MKK1; MAPK kinase) and the closely related MKK2. It has anti-cancer activity, suppresses the ERK pathway, and has been used along with other classes of inhibitors to establish embryonic stem cell lines.
storage
Store at +4°C
References
[1] frémin c, meloche s. from basic research to clinical development of mek1/2 inhibitors for cancer therapy. j hematol oncol. 2010 feb 11;3:8. doi: 10.1186/1756-8722-3-8.
Properties of PD184352
Melting point: | 166-169°C |
Density | 1.747±0.06 g/cm3(Predicted) |
storage temp. | room temp |
solubility | DMSO: ≥30mg/mL |
pka | -5.58±0.50(Predicted) |
form | powder |
color | white to tan |
Safety information for PD184352
Signal word | Warning |
Pictogram(s) |
Environment GHS09 |
GHS Hazard Statements |
H400:Hazardous to the aquatic environment, acute hazard |
Precautionary Statement Codes |
P273:Avoid release to the environment. |
Computed Descriptors for PD184352
New Products
6-Bromo 2-Iodo Indole Pyridine 2,4,6-Tricarboxaldehyde Fosfomycin EP impurity D Rimegepant Impurity 3 Ivermectin EP Impurity B Tubulysin B (R)-tert-butyl (4-methyl-1-oxopentan-3-yl)carbamate Tubulysin G Tubulysin F 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate Fuel shell 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol Imeglimin Hydrochloride IH (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine Calcium Sodium Phosphosilicate IH 2-(2,4-Dibutoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane 1-(4-Aminophenyl)-3-morpholino-5,6-dihydropyridin-2(1H)-one 3,3,6,6-Tetramethylcyclohexane-1,2-dione Methyl 4-amino-3-(pyrrolidin-1-yl)benzoate 1-(4-Fluorophenyl)piperidin-2-one 3,6-Bis(4-iodophenyl)-2,5-dihydropyrrolo[3,4-c]pyrrole-1,4-dione 1,3,5-Trimethyl-1,4-cyclohexadiene (-)-1-Phenyl ethane sulfonic acid 6-HydroxyisoquinolineRelated products of tetrahydrofuran
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