WX-554

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

MedKoo CAT#: 206012

CAS#: 945529-91-9

Description: WX-554 is an orally available small molecule mitogen-activated protein kinase kinase (MAP2K, MAPK/ERK kinase, or MEK) inhibitor, with potential antineoplastic activity. MEK inhibitor WX-554 selectively binds to and inhibits the activity of MEK, thereby preventing the activation of MEK-dependent effector proteins including some transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK, a dual-specificity threonine/tyrosine kinase that plays a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway, is frequently upregulated in a variety of tumor cell types.

Chemical Structure

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WX-554
CAS# 945529-91-9
Instruction

Theoretical Analysis

MedKoo Cat#: 206012
Name: WX-554
CAS#: 945529-91-9
Chemical Formula: C18H16FIN4OS
Exact Mass: 482.01
Molecular Weight: 482.320
Elemental Analysis: C, 44.82; H, 3.34; F, 3.94; I, 26.31; N, 11.62; O, 3.32; S, 6.65

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: WX554; WX-554; WX 554.

IUPAC/Chemical Name: [3-(aminomethyl)azetidin-1-yl]-{2-[(2-fluoro-4-iodophenyl)amino]thieno[2,3-b]pyridin-3-yl}-methanone

InChi Key: DJIBEZXMCYNIQJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H16FIN4OS/c19-13-6-11(20)3-4-14(13)23-17-15(12-2-1-5-22-16(12)26-17)18(25)24-8-10(7-21)9-24/h1-6,10,23H,7-9,21H2

SMILES Code: O=C(N1CC(CN)C1)C2=C(NC3=CC=C(I)C=C3F)SC4=NC=CC=C42

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: >5 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:         

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 482.32 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:
In vitro protocol:
In vivo protocol:

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 1: Ghanaatgar-Kasbi S, Khazaei M, Rastgar-Moghadam A, Ferns GA, Hassanian SM, Avan A. The Therapeutic Potential of MEK1/2 Inhibitors in the Treatment of Gynecological Cancers: Rational Strategies and Recent Progress. Curr Cancer Drug Targets. 2020;20(6):417-428. doi: 10.2174/1568009620666200424144303. PMID: 32329688.


2: Haagensen EJ, Thomas HD, Schmalix WA, Payne AC, Kevorkian L, Allen RA, Bevan P, Maxwell RJ, Newell DR. Enhanced anti-tumour activity of the combination of the novel MEK inhibitor WX-554 and the novel PI3K inhibitor WX-037. Cancer Chemother Pharmacol. 2016 Dec;78(6):1269-1281. doi: 10.1007/s00280-016-3186-4. Epub 2016 Nov 11. PMID: 27837257; PMCID: PMC5114336.


3: Jamieson D, Griffin MJ, Sludden J, Drew Y, Cresti N, Swales K, Merriman M, Allen R, Bevan P, Buerkle M, Mala C, Coyle V, Rodgers L, Dean E, Greystoke A, Banerji U, Wilson RH, Evans TR, Anthoney A, Ranson M, Boddy AV, Plummer R. A phase I pharmacokinetic and pharmacodynamic study of the oral mitogen-activated protein kinase kinase (MEK) inhibitor, WX-554, in patients with advanced solid tumours. Eur J Cancer. 2016 Nov;68:1-10. doi: 10.1016/j.ejca.2016.08.026. Epub 2016 Sep 28. PMID: 27693888.


4: Miller CR, Oliver KE, Farley JH. MEK1/2 inhibitors in the treatment of gynecologic malignancies. Gynecol Oncol. 2014 Apr;133(1):128-37. doi: 10.1016/j.ygyno.2014.01.008. Epub 2014 Jan 14. PMID: 24434059.


5: Akinleye A, Furqan M, Mukhi N, Ravella P, Liu D. MEK and the inhibitors: from bench to bedside. J Hematol Oncol. 2013 Apr 12;6:27. doi: 10.1186/1756-8722-6-27. PMID: 23587417; PMCID: PMC3626705.