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PD184352

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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
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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
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Safety Information

Hazard Codes 
N
Risk Statements 
50/53
Safety Statements 
60-61
RIDADR 
UN 3077 9 / PGIII
WGK Germany 
3
HS Code 
2924297099
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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.

PD184352Supplier

Shanghai Boyle Chemical Co., Ltd.
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J & K SCIENTIFIC LTD.
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Chemsky(shanghai)International Co.,Ltd.
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Jinan Trio PharmaTech Co., Ltd.
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