PD 98059 | PD098059 | CAS#167869-21-8 | MARK/MEK inhibitor

MedKoo Cat#: 401680 | Name: PD98059

Description:

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

PD98059 also known as PD-98059, is a potent and selective inhibitor of MAP kinase kinase (also known as MAPK/ERK kinase or MEK kinase). It mediates its inhibitory properties by binding to the ERK-specific MAP kinase MEK, therefore preventing phosphorylation of ERK1/2 (p44/p42 MAPK) by MEK1/2. MAPK ERK1/2 is involved in TLR-induced production of cytokines.

Chemical Structure

PD98059

CAS#167869-21-8

Theoretical Analysis

MedKoo Cat#: 401680

Name: PD98059

CAS#: 167869-21-8

Chemical Formula: C16H13NO3

Exact Mass: 267.0895

Molecular Weight: 267.28

Elemental Analysis: C, 71.90; H, 4.90; N, 5.24; O, 17.96

Price and Availability

Size	Price	Availability
10mg	USD 90.00	Ready to ship
25mg	USD 150.00	Ready to ship
50mg	USD 250.00	Ready to ship
100mg	USD 450.00	Ready to ship
200mg	USD 800.00	Ready to ship
500mg	USD 1,750.00	Ready to ship
1g	USD 2,950.00	Ready to ship

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Related CAS #

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Synonym

PD98059; PD-98059; PD 98059; PD098059

IUPAC/Chemical Name

2-(2-amino-3-methoxyphenyl)-4H-chromen-4-one

InChi Key

QFWCYNPOPKQOKV-UHFFFAOYSA-N

InChi Code

InChI=1S/C16H13NO3/c1-19-14-8-4-6-11(16(14)17)15-9-12(18)10-5-2-3-7-13(10)20-15/h2-9H,17H2,1H3

SMILES Code

O=C1C=C(C2=CC=CC(OC)=C2N)OC3=C1C=CC=C3

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, not in water

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

Certificate of Analysis

View CoA: current batch, Lot#A8T09K05

View CoA: current batch, Lot#A8T09K26

QC Data

View QC data: current batch, Lot#A8T09K05

View QC data: current batch, Lot#A8T09K26

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

PD98059 is a MEK inhibitor with an IC50 of 5 µM.

In vitro activity:

To determine the antiproliferative effects of PD98059 on breast cancer cells, MCF-7 and MDA-MB-231 breast cancer cells were treated with 1, 5, 10 and 20 µM PD98059 for 24 h. As shown in Fig. 1A and B, after incubation of the MCF-7 and MDA-MB-231 cells with 1, 5, 10 and 20 µM PD98059 for 24 h, the expression of phosphorylated MEK1 which is an indicator of MEK1 activation was markedly decreased from 5 to 20 µM compared with the control group. PD98059 inhibited MCF-7 and MDA-MB-231 cell proliferation in a dose-dependent manner using MTT assay (Fig. 1C and D). For example, the cell growth inhibition ratio was increased from 4.7% at the dose of 1 µM to 33.1% at the dose of 50 µM in MCF-7 breast cancer cells. Similarly, the cell growth inhibition ratio was increased from 4.2% at the dose of 1 µM to 40.5% at the dose of 50 µM in the MDA-MB-231 breast cancer cells. Reference: Oncol Rep. 2017 Nov;38(5):3055-3063. https://www.spandidos-publications.com/or/38/5/3055

In vivo activity:

In CCI (chronic constriction injury) exposed rats single intrathecal PD98059 (2.5 mcg) administration produced significant antiallodynic effect after 30 min as assessed at day 7 by the von Frey test (18.5 g ± 0.55, n = 10; Fig 4C and 4D). Single intrathecal PD98059 (2.5 mcg) administration enhanced morphine-induced analgesia (24.2 ± 0.63, n = 8, Fig 4C). Single intrathecal PD98059 (2.5 mcg) administration also enhanced buprenorphine-induced analgesia (23.25 ± 0.62, n = 7, Fig 4D). Reference: PLoS One. 2015 Oct 1;10(10):e0138583. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4591269/

	Solvent	mg/mL	mM
Solubility
	DMSO	15.0	56.10

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 267.28 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.

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. Zhao Y, Ge CC, Wang J, Wu XX, Li XM, Li W, Wang SS, Liu T, Hou JZ, Sun H, Fang D, Xie SQ. MEK inhibitor, PD98059, promotes breast cancer cell migration by inducing β-catenin nuclear accumulation. Oncol Rep. 2017 Nov;38(5):3055-3063. doi: 10.3892/or.2017.5955. Epub 2017 Sep 13. PMID: 29048617. 2. Rojewska E, Popiolek-Barczyk K, Kolosowska N, Piotrowska A, Zychowska M, Makuch W, Przewlocka B, Mika J. PD98059 Influences Immune Factors and Enhances Opioid Analgesia in Model of Neuropathy. PLoS One. 2015 Oct 1;10(10):e0138583. doi: 10.1371/journal.pone.0138583. PMID: 26426693; PMCID: PMC4591269.

In vitro protocol:

In vivo protocol:

1. Rojewska E, Popiolek-Barczyk K, Kolosowska N, Piotrowska A, Zychowska M, Makuch W, Przewlocka B, Mika J. PD98059 Influences Immune Factors and Enhances Opioid Analgesia in Model of Neuropathy. PLoS One. 2015 Oct 1;10(10):e0138583. doi: 10.1371/journal.pone.0138583. PMID: 26426693; PMCID: PMC4591269.

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