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PD 184161

Product Name
PD 184161
CAS No.
212631-67-9
Chemical Name
PD 184161
Synonyms
PD 184161;UK-287074;PF-3011370;PF-1529483;MEK1/2 Inhibitor IV;MEK1/2 Inhibitor IV - CAS 212631-67-9 - Calbiochem;5-BroMo-2-[(2-chloro-4-iodophenyl)aMino]-N-(cyclopropylMethoxy)-3,4-difluorobenzaMide;Benzamide, 5-bromo-2-[(2-chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluoro-;MAP2K,PD-184161,cell,Apoptosis,neurons,Mitogen-activated protein kinase kinase,stroke,PD184161,depressive,PD 184161,cancer,HCC,MAPKK,Inhibitor,inhibit,MEK,behavioral
CBNumber
CB02545547
Molecular Formula
C17H13BrClF2IN2O2
Formula Weight
557.56
MOL File
212631-67-9.mol
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PD 184161 Property

Melting point:
174-175 °C
Density 
1.922±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO: >10mg/mL
pka
-6.25±0.50(Predicted)
form 
White solid
color 
white to off-white
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

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.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
PZ0112
Product name
PD-184161
Purity
≥98% (HPLC)
Packaging
5mg
Price
$150
Updated
2024/03/01
Sigma-Aldrich
Product number
444967
Product name
MEK1/2 Inhibitor IV
Packaging
5mg
Price
$230
Updated
2024/03/01
Cayman Chemical
Product number
10012431
Product name
PD 184161
Purity
≥98%
Packaging
1mg
Price
$28
Updated
2024/03/01
Cayman Chemical
Product number
10012431
Product name
PD 184161
Purity
≥98%
Packaging
5mg
Price
$117
Updated
2024/03/01
Sigma-Aldrich
Product number
PZ0112
Product name
PD-184161
Purity
≥98% (HPLC)
Packaging
25mg
Price
$477
Updated
2024/03/01
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PD 184161 Chemical Properties,Usage,Production

Chemical Properties

Off-White Solid

Uses

A novel mitogen-activated protein kinase kinase (MEK) inhibitor shown to exhibit antitumor effects and suppress MEK-extracellular signal-related kinase signaling activity and cell proliferation in human hepatocellular carcinoma cells and in human hepatocellular carcinoma xenografts.

General Description

A cell-permeable, blood-brain barrier permeant, and orally active hydroxamate compound that is reported to inhibit MEK activity (IC50 = 10-100 nM) without competing against ATP or Erk binding and exhibit excellent selectivity over 27 other cellular kinases, including JNK, MAPK2/ERK2, SAPK2a, SAPK2b, SAPK3, and SAPK4 (IC50 >10 M). Shown to be superior to PD 98059 and U0126 in suppressing Erk1/2 phosphorylation in Hep3B, HepG2, PLC, and SKHep human liver cancer cells (IC50<0.1 M) in vitro and effectively reduce Erk1/2 phosphorylation in hippocampal tissue in mice (ED50<50 mg/kg, i.p.) in vivo. Both PD184161 and U0126 are shown to induce necrosis of several types of glucose-deprived cells via an indirect action on the F0 component of the mitochondrial F1F0-ATPase/synthase.

Biological Activity

pd 184161 is a mek1/2 inhibitor.the intracellular signaling pathway of mitogen-activated protein kinases is involved in the regulation of various cellular functions. one of these pathways, named raf/mek/erk pathway, plays a key role in the regulation of cellular differentiation, growth, and proliferation. the modulation of this raf/mek/erk pathway has been reported as a useful approach to treate proliferative disorders such as cancer.

Biochem/physiol Actions

PD-184161 is a MEK inhibitor.

in vitro

previous study found that pd184161 could inhibit mek activity in a time- and concentration-dependent manner, which was more effectively than pd098059 or u0126. moreover, pd184161 could inhibit cell proliferation and induce apoptosis at concentrations of > or = 1.0 μm time- and concentration-dependently [1].

in vivo

animal study showd that tumor xenograft p-erk levels were significantly reduced 3 to 12 hours after an oral dose of pd184161. contrarily, tumor xenograft p-erk levels following long-term treatment of pd184161 were refractory to this signaling effect. pd184161 also significantly suppressed tumor engraftment and initial growth, however, established tumors were not significantly affected. in summary, pd184161 has antitumor effects in hcc in vivo that appear to correlate with suppression of mek activity [1].

IC 50

10-100 nm

References

[1] klein, p. j.,schmidt, c.m.,wiesenauer, c.a., et al. the effects of a novel mek inhibitor pd184161 on mek-erk signaling and growth in human liver cancer. neoplasia 8(1), 1-8 (2006).

PD 184161 Preparation Products And Raw materials

Raw materials

Preparation Products

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PD 184161 Suppliers

Canada 1 China 40 India 1 United States 5 Global 47
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
Chemsky（shanghai）International Co.,Ltd.
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
32344
Advantage
50
Tianjin Anhao Biological Technology Co., Ltd.
Tel
Email
sales@ahpharmatech.com
Country
China
ProdList
5738
Advantage
55
Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Country
China
ProdList
51471
Advantage
80
Tianjin Kailiqi Biotechnology Co., Ltd.
Tel
15076683720
Fax
022-23754520
Email
klq@cw-bio.com
Country
China
ProdList
3501
Advantage
55
ShangHai Biochempartner Co.,Ltd
Tel
17754423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8011
Advantage
62
Aikon International Limited
Tel
025-58851090 13611564524
Fax
(6)02557626880
Email
lwan@aikonchem.com
Country
China
ProdList
15952
Advantage
58
Shenzhen Polymeri Biochemical Technology Co., Ltd.
Tel
+86-400-002-6226 13028896684
Email
sales@rrkchem.com
Country
China
ProdList
55896
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
Country
United States
ProdList
19892
Advantage
58
DC Chemicals
Tel
021-58447131 13564518121
Email
sales@dcchemicals.com
Country
China
ProdList
9414
Advantage
58

212631-67-9, PD 184161Related Search:


  • PD 184161
  • PF-1529483
  • PF-3011370
  • UK-287074
  • MEK1/2 Inhibitor IV
  • 5-BroMo-2-[(2-chloro-4-iodophenyl)aMino]-N-(cyclopropylMethoxy)-3,4-difluorobenzaMide
  • MEK1/2 Inhibitor IV - CAS 212631-67-9 - Calbiochem
  • Benzamide, 5-bromo-2-[(2-chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluoro-
  • MAP2K,PD-184161,cell,Apoptosis,neurons,Mitogen-activated protein kinase kinase,stroke,PD184161,depressive,PD 184161,cancer,HCC,MAPKK,Inhibitor,inhibit,MEK,behavioral
  • 212631-67-9
  • C17H13BrClF2IN2O2
  • Amines
  • Aromatics
  • Intermediates & Fine Chemicals
  • Pfizer compounds
  • Pharmaceuticals
  • Protein Kinase Inhibitors and Activators