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
- Product Categories:
-
- Anti-cancer&immunity
- MAPK
- Pfizer compounds
- Amines
- Aromatics
- Intermediates & Fine Chemicals
- All Inhibitors
- Inhibitors
- Pharmaceuticals
- Mol File:
- 212631-79-3.mol
PD184352 Chemical Properties
- 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
PD184352 Usage And Synthesis
Chemical Properties
Off-White to Pale Beige Solid
Uses
An inhibitor of ERK signaling pathway. A MAP kinase inhibitor. Potent 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.
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