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MedKoo Cat#: 206012 | Name: WX-554

Description:

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

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

WX-554
WX-554
CAS#945529-91-9

Theoretical Analysis

MedKoo Cat#: 206012

Name: WX-554

CAS#: 945529-91-9

Chemical Formula: C18H16FIN4OS

Exact Mass: 482.0074

Molecular Weight: 482.32

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 currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
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
        

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
 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.