PD184161

Modify Date: 2024-01-21 21:07:23

PD184161 Structure
PD184161 structure
Common Name PD184161
CAS Number 212631-67-9 Molecular Weight 557.556
Density 1.9±0.1 g/cm3 Boiling Point N/A
Molecular Formula C17H13BrClF2IN2O2 Melting Point N/A
MSDS USA Flash Point N/A
Symbol GHS09
GHS09
Signal Word Warning

 Use of PD184161


PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior[1][2].

 Names

Name 5-bromo-2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide
Synonym More Synonyms

 PD184161 Biological Activity

Description PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior[1][2].
Related Catalog
Target

MEK:10-100 nM (IC50)

In Vitro PD184161 (1-20 μM; 24, 48, or 72 hours) inhibits cell proliferation and induces apoptosis in a time and concentration dependent manner[1]. PD184161 (0.1 and 1.0 μM; 1 hour) inhibits ERK1,2 phosphorylation[1]. PD184161 (5 μM; 30 min) prevents the toxic effects of bicuculline[3]. Cell Proliferation Assay[1] Cell Line: HCC cell lines (HepG2, Hep3B, PLC, and SKHep) Concentration: 1-20 μM Incubation Time: 24, 48, or 72 hours Result: Inhibited cell proliferation. Apoptosis Analysis[1] Cell Line: HCC cell lines (HepG2, Hep3B, PLC, and SKHep) Concentration: 1-20 μM Incubation Time: 48 hours Result: Induced cell apoptosis. Western Blot Analysis[1] Cell Line: HCC cell lines (HepG2, Hep3B, PLC, and SKHep) Concentration: 0.1 and 1.0 μM Incubation Time: 1 hours Result: Inhibited ERK1,2 phosphorylation. Cell Viability Assay[3] Cell Line: Primary mouse neurons Concentration: 5 μM Incubation Time: 30 min Result: Prevents the toxic effects of bicuculline.
In Vivo PD184161 reduces tumor xenograft P-ERK levels in 3-12 hours after an oral dose[1]. PD184161 (300 mg/kg; orogastric gavage twice daily for 38 days) significantly suppresses tumor engraftment and initial growth[1]. PD184161 (30 mg/kg; i.p.; single injection) produces depressive-like behavior[2]. PD184161 (500 μg/kg; intravenous injection) prevents the progression of neurological deficits and brain damage after stroke[3]. Animal Model: Hep3B tumor xenografts BALB/c athymic nude mice[1] Dosage: 300 mg/kg Administration: Orogastric gavage twice daily for 38 days Result: Decreased the early tumor growth. Animal Model: Male, 6 weeks C57Bl/6 mice[2] Dosage: 500 μg/kg Administration: intravenously in 30 min before MCAO or PTZ administration Result: Prevented the progression of neurological deficits and brain damage after stroke. Animal Model: C57Bl/6 mice[3] Dosage: 30 mg/kg Administration: i.p., single injection Result: Produced depressive-like behavior.
References

[1]. Klein PJ, et al. The effects of a novel MEK inhibitor PD184161 on MEK-ERK signaling and growth in human liver cancer. Neoplasia. 2006 Jan;8(1):1-8.

[2]. Duman CH, et al. A role for MAP kinase signaling in behavioral models of depression and antidepressant treatment. Biol Psychiatry. 2007 Mar 1;61(5):661-70.

[3]. Gladbach A, et al. ERK inhibition with PD184161 mitigates brain damage in a mouse model of stroke. J Neural Transm (Vienna). 2014 May;121(5):543-7.

 Chemical & Physical Properties

Density 1.9±0.1 g/cm3
Molecular Formula C17H13BrClF2IN2O2
Molecular Weight 557.556
Exact Mass 555.886169
PSA 50.36000
LogP 9.28
Index of Refraction 1.670

 Safety Information

Symbol GHS09
GHS09
Signal Word Warning
Hazard Statements H400
Precautionary Statements P273
RIDADR UN 3077 9 / PGIII

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 Synonyms

Benzamide, 5-bromo-2-[(2-chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluoro-
5-Bromo-2-[(2-chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluorobenzamide
hms3263a07
PD 184161
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