PD184352

PD184352 Basic information
Product Name:PD184352
Synonyms:CI1040;PD-184352; CI 1040 (PD184352);CS-333;PD184352;2-[(2-Chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluorobenzamide;2-(2-CHLORO-4-IODOANILINO)-N-(CYCLOPROPYLMETHOXY)-3,4-DIFLUOROBENZAMIDE;2-[(2-CHLORO-4-IODOPHENYL) AMINO]-N-(CYCLOPROPYLME;Benzamide, 2-[(2-chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluoro-;Ci-1040
CAS:212631-79-3
MF:C17H14ClF2IN2O2
MW:478.66
EINECS:
Product Categories:Anti-cancer&immunity;MAPK;Pfizer compounds;Amines;Aromatics;Intermediates & Fine Chemicals;All Inhibitors;Inhibitors;Pharmaceuticals
Mol File:212631-79-3.mol
PD184352 Structure
PD184352 Chemical Properties
Melting point 166-169°C
density 1.747±0.06 g/cm3(Predicted)
storage temp. room temp
solubility DMSO: ≥30mg/mL
form powder
pka-5.58±0.50(Predicted)
color white to tan
Safety Information
Hazard Codes N
Risk Statements 50/53
Safety Statements 60-61
RIDADR UN 3077 9 / PGIII
WGK Germany 3
HS Code 2924297099
MSDS Information
PD184352 Usage And Synthesis
Chemical PropertiesOff-White to Pale Beige Solid
UsesAn inhibitor of ERK signaling pathway. A MAP kinase inhibitor. Potent MEK inhibitor.
DefinitionChEBI: 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide is an aminobenzoic acid.
Biological Activitypd184352 (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 ActionsPD184352 (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.
storageStore 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.
PD184352 Preparation Products And Raw materials
Rapamycin CHIR-99021 LY 294002 HYDROCHLORIDE SB 203580 Trametinib Selumetinib CHLOROPHENYLSILANE 97 Phenyl carbamate PD184352 (CI-1040) Benzenemethanamine, 2-amino-4-fluoro- (9CI) 2-Chloro-4-iodoaniline PD184352/CI-1040 CYCLOPROPYL METHOXYLAMINE HYDROCHLORIDE 2-FLUORODIPHENYLAMINE 2-[(2-Chlorophenyl)amino]-benzaldehyde 1-Chloro-3-iodobenzene 4-fluoro-N-hydroxybenzamide 3-FLUORODIPHENYLAMINE

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