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MedKoo Cat#: 406196 | Name: PD184161
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PD184161 is an orally-active MEK inhibitor. PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner more effectively than PD098059 or U0126. PD184161 inhibited cell proliferation and induced apoptosis at concentrations of > or = 1.0 microM in a time- and concentration-dependent manner. PD184161 has antitumor effects in HCC in vitro and in vivo that appear to correlate with suppression of MEK activity. PD184161 is unable to suppress MEK activity in HCC xenografts in the long term.

Chemical Structure

PD184161
PD184161
CAS#212631-67-9

Theoretical Analysis

MedKoo Cat#: 406196

Name: PD184161

CAS#: 212631-67-9

Chemical Formula: C17H13BrClF2IN2O2

Exact Mass: 555.8862

Molecular Weight: 557.56

Elemental Analysis: C, 36.62; H, 2.35; Br, 14.33; Cl, 6.36; F, 6.81; I, 22.76; N, 5.02; O, 5.74

Price and Availability

Size Price Availability Quantity
5mg USD 450.00
10mg USD 700.00
25mg USD 1,050.00
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Related CAS #
No Data
Synonym
PD184161; PD 184161; PD184161; PF1529483 PF3011370 UK287074.
IUPAC/Chemical Name
2-(2-chloro-4-iodophenylamino)-N-cyclopropylmethoxy-3,4-difluoro-5-bromobenzamide
InChi Key
VJNZMSLGVUSPCF-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H13BrClF2IN2O2/c18-11-6-10(17(25)24-26-7-8-1-2-8)16(15(21)14(11)20)23-13-4-3-9(22)5-12(13)19/h3-6,8,23H,1-2,7H2,(H,24,25)
SMILES Code
O=C(NOCC1CC1)C2=CC(Br)=C(F)C(F)=C2NC3=CC=C(I)C=C3Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
        
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PD184161 is an orally active MEK inhibitor.
In vitro activity:
PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner more effectively than PD098059 or U0126. PD184161 inhibited cell proliferation and induced apoptosis at concentrations of > or = 1.0 microM in a time- and concentration-dependent manner. Reference: Neoplasia. 2006 Jan;8(1):1-8. https://pubmed.ncbi.nlm.nih.gov/16533420/
In vivo activity:
This study examined the effects of inhibition of MAPK kinase (MEK) in mouse behavioral models for depression including interactions with effects of antidepressant drugs. Acute administration of the MEK inhibitor PD184161 produced depressive-like behavior. PD184161 blocked the antidepressant-like effects of desipramine and sertraline in the forced swim test and blocked the effects of desipramine in the tail suspension test. Reference: Biol Psychiatry. 2007 Mar 1;61(5):661-70. https://pubmed.ncbi.nlm.nih.gov/16945347/
Solvent mg/mL mM
Solubility
DMF 30.0 53.81
DMSO 75.3 135.11
DMSO:PBS (pH 7.2) (1:2) 0.3 0.54
Ethanol 12.0 21.52
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 557.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Pellicano F, Simara P, Sinclair A, Helgason GV, Copland M, Grant S, Holyoake TL. The MEK inhibitor PD184352 enhances BMS-214662-induced apoptosis in CD34+ CML stem/progenitor cells. Leukemia. 2011 Jul;25(7):1159-67. doi: 10.1038/leu.2011.67. Epub 2011 Apr 12. PMID: 21483442; PMCID: PMC3643208. 2. Klein PJ, Schmidt CM, Wiesenauer CA, Choi JN, Gage EA, Yip-Schneider MT, Wiebke EA, Wang Y, Omer C, Sebolt-Leopold JS. 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. doi: 10.1593/neo.05373. PMID: 16533420; PMCID: PMC1601146. 3. Gladbach A, van Eersel J, Bi M, Ke YD, Ittner LM. ERK inhibition with PD184161 mitigates brain damage in a mouse model of stroke. J Neural Transm (Vienna). 2014 May;121(5):543-7. doi: 10.1007/s00702-013-1138-2. Epub 2013 Dec 14. PMID: 24337667. 4. Duman CH, Schlesinger L, Kodama M, Russell DS, Duman RS. A role for MAP kinase signaling in behavioral models of depression and antidepressant treatment. Biol Psychiatry. 2007 Mar 1;61(5):661-70. doi: 10.1016/j.biopsych.2006.05.047. Epub 2006 Aug 30. PMID: 16945347.
In vitro protocol:
1. Pellicano F, Simara P, Sinclair A, Helgason GV, Copland M, Grant S, Holyoake TL. The MEK inhibitor PD184352 enhances BMS-214662-induced apoptosis in CD34+ CML stem/progenitor cells. Leukemia. 2011 Jul;25(7):1159-67. doi: 10.1038/leu.2011.67. Epub 2011 Apr 12. PMID: 21483442; PMCID: PMC3643208. 2. Klein PJ, Schmidt CM, Wiesenauer CA, Choi JN, Gage EA, Yip-Schneider MT, Wiebke EA, Wang Y, Omer C, Sebolt-Leopold JS. 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. doi: 10.1593/neo.05373. PMID: 16533420; PMCID: PMC1601146.
In vivo protocol:
1. Gladbach A, van Eersel J, Bi M, Ke YD, Ittner LM. ERK inhibition with PD184161 mitigates brain damage in a mouse model of stroke. J Neural Transm (Vienna). 2014 May;121(5):543-7. doi: 10.1007/s00702-013-1138-2. Epub 2013 Dec 14. PMID: 24337667. 2. Duman CH, Schlesinger L, Kodama M, Russell DS, Duman RS. A role for MAP kinase signaling in behavioral models of depression and antidepressant treatment. Biol Psychiatry. 2007 Mar 1;61(5):661-70. doi: 10.1016/j.biopsych.2006.05.047. Epub 2006 Aug 30. PMID: 16945347.
1: Matsushita H, Matsuzaki M, Han XJ, Nishiki TI, Ohmori I, Michiue H, Matsui H, Tomizawa K. Antidepressant-like effect of sildenafil through oxytocin-dependent cyclic AMP response element-binding protein phosphorylation. Neuroscience. 2012 Jan 3;200:13-8. doi: 10.1016/j.neuroscience.2011.11.001. Epub 2011 Nov 9. PubMed PMID: 22088430. 2: Mazharian A, Watson SP, Séverin S. Critical role for ERK1/2 in bone marrow and fetal liver-derived primary megakaryocyte differentiation, motility, and proplatelet formation. Exp Hematol. 2009 Oct;37(10):1238-1249.e5. doi: 10.1016/j.exphem.2009.07.006. Epub 2009 Jul 18. PubMed PMID: 19619605; PubMed Central PMCID: PMC2755112. 3: Yip-Schneider MT, Klein PJ, Wentz SC, Zeni A, Menze A, Schmidt CM. Resistance to mitogen-activated protein kinase kinase (MEK) inhibitors correlates with up-regulation of the MEK/extracellular signal-regulated kinase pathway in hepatocellular carcinoma cells. J Pharmacol Exp Ther. 2009 Jun;329(3):1063-70. doi: 10.1124/jpet.108.147306. Epub 2009 Mar 3. PubMed PMID: 19258520. 4: Choi J, Yip-Schneider M, Albertin F, Wiesenauer C, Wang Y, Schmidt CM. The effect of doxorubicin on MEK-ERK signaling predicts its efficacy in HCC. J Surg Res. 2008 Dec;150(2):219-26. doi: 10.1016/j.jss.2008.01.029. Epub 2008 Mar 3. PubMed PMID: 18468633. 5: Duman CH, Schlesinger L, Russell DS, Duman RS. Voluntary exercise produces antidepressant and anxiolytic behavioral effects in mice. Brain Res. 2008 Mar 14;1199:148-58. doi: 10.1016/j.brainres.2007.12.047. Epub 2008 Jan 3. Erratum in: Brain Res. 2008 Jul 7;1218:313. PubMed PMID: 18267317; PubMed Central PMCID: PMC2330082. 6: Duman CH, Schlesinger L, Kodama M, Russell DS, Duman RS. A role for MAP kinase signaling in behavioral models of depression and antidepressant treatment. Biol Psychiatry. 2007 Mar 1;61(5):661-70. Epub 2006 Aug 30. PubMed PMID: 16945347. 7: Klein PJ, Schmidt CM, Wiesenauer CA, Choi JN, Gage EA, Yip-Schneider MT, Wiebke EA, Wang Y, Omer C, Sebolt-Leopold JS. 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. PubMed PMID: 16533420; PubMed Central PMCID: PMC1601146. 8: Thottassery JV, Sun Y, Westbrook L, Rentz SS, Manuvakhova M, Qu Z, Samuel S, Upshaw R, Cunningham A, Kern FG. Prolonged extracellular signal-regulated kinase 1/2 activation during fibroblast growth factor 1- or heregulin beta1-induced antiestrogen-resistant growth of breast cancer cells is resistant to mitogen-activated protein/extracellular regulated kinase kinase inhibitors. Cancer Res. 2004 Jul 1;64(13):4637-47. PubMed PMID: 15231676. 9: Yung HW, Wyttenbach A, Tolkovsky AM. Aggravation of necrotic death of glucose-deprived cells by the MEK1 inhibitors U0126 and PD184161 through depletion of ATP. Biochem Pharmacol. 2004 Jul 15;68(2):351-60. PubMed PMID: 15194007. 10: Marshall SJ, Senis YA, Auger JM, Feil R, Hofmann F, Salmon G, Peterson JT, Burslem F, Watson SP. GPIb-dependent platelet activation is dependent on Src kinases but not MAP kinase or cGMP-dependent kinase. Blood. 2004 Apr 1;103(7):2601-9. Epub 2003 Dec 18. PubMed PMID: 14684423.