GW843682X | CAS3660868-91-7 | PLK1 inhibitor

GW843682X
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406798

CAS#: 660868-91-7

Description: GW843682X is a selective inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3) (IC50 values are 2.2 and 9.1 nM respectively). GW843682X inhibited the proliferation and induced apoptosis of 5-8F cells in a dose-dependent manner (IC50=62.5-125nmol/L). GW843682X exhibited remarkable cytotoxic effects on nasopharyngeal carcinoma 5-8F cells by down-regulating IAP gene expression, suggesting that GW843682X may become a novel therapeutic agent for nasopharyngeal carcinoma.

Chemical Structure

GW843682X

CAS# 660868-91-7

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406798
Name: GW843682X
CAS#: 660868-91-7
Chemical Formula: C22H18F3N3O4S
Exact Mass: 477.10
Molecular Weight: 477.458
Elemental Analysis: C, 55.34; H, 3.80; F, 11.94; N, 8.80; O, 13.40; S, 6.71

Price and Availability

Size	Price	Availability
5mg	USD 300	2 Weeks
10mg	USD 550	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: GW843682X; GW 843682X; GW-843682X.

IUPAC/Chemical Name: 5-(5,6-dimethoxybenzimidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]thiophene-2-carboxamide

InChi Key: JSKUWFIZUALZLX-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H18F3N3O4S/c1-30-16-7-14-15(8-17(16)31-2)28(11-27-14)19-9-18(20(33-19)21(26)29)32-10-12-5-3-4-6-13(12)22(23,24)25/h3-9,11H,10H2,1-2H3,(H2,26,29)

SMILES Code: O=C(C1=C(OCC2=CC=CC=C2C(F)(F)F)C=C(N3C4=CC(OC)=C(OC)C=C4N=C3)S1)N

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:	GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ∼30 other kinases.
In vitro activity:	The qRT-PCR and ELISA results showed that GW843682X down-regulated the expression of TNF-α induced by Pam3CSK4 or LPS and the expression of IL-8 induced by LPS at both the gene and protein levels (Figures 2A-D), but it did not affect the expression of IL-1β induced by Pam3CSK4 or LPS, or the expression of IL-8 induced by Pam3CSK4 (Figures 2A-D). Reference: PLoS One. 2013 Oct 18;8(10):e78832. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3799749/
In vivo activity:	TBD

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	36.4	76.20
	Ethanol	3.2	6.69

Preparing Stock Solutions

The following data is based on the product molecular weight 477.46 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. Hu J, Wang G, Liu X, Zhou L, Jiang M, Yang L. Polo-like kinase 1 (PLK1) is involved in toll-like receptor (TLR)-mediated TNF-α production in monocytic THP-1 cells. PLoS One. 2013 Oct 18;8(10):e78832. doi: 10.1371/journal.pone.0078832. PMID: 24205328; PMCID: PMC3799749. 2. Ikezoe T, Yang J, Nishioka C, Takezaki Y, Tasaka T, Togitani K, Koeffler HP, Yokoyama A. A novel treatment strategy targeting polo-like kinase 1 in hematological malignancies. Leukemia. 2009 Sep;23(9):1564-76. doi: 10.1038/leu.2009.94. Epub 2009 May 7. PMID: 19421227.
In vitro protocol:	1. Hu J, Wang G, Liu X, Zhou L, Jiang M, Yang L. Polo-like kinase 1 (PLK1) is involved in toll-like receptor (TLR)-mediated TNF-α production in monocytic THP-1 cells. PLoS One. 2013 Oct 18;8(10):e78832. doi: 10.1371/journal.pone.0078832. PMID: 24205328; PMCID: PMC3799749. 2. Ikezoe T, Yang J, Nishioka C, Takezaki Y, Tasaka T, Togitani K, Koeffler HP, Yokoyama A. A novel treatment strategy targeting polo-like kinase 1 in hematological malignancies. Leukemia. 2009 Sep;23(9):1564-76. doi: 10.1038/leu.2009.94. Epub 2009 May 7. PMID: 19421227.
In vivo protocol:	TBD

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1: Hu Q, Chu Y, Hu W, Peng M, Song Q. The cytotoxic effect of GW843682X on nasopharyngeal carcinoma. Anticancer Agents Med Chem. 2016 May 20. [Epub ahead of print] PubMed PMID: 27198987.

2: Hu J, Wang G, Liu X, Zhou L, Jiang M, Yang L. Polo-like kinase 1 (PLK1) is involved in toll-like receptor (TLR)-mediated TNF-α production in monocytic THP-1 cells. PLoS One. 2013 Oct 18;8(10):e78832. doi: 10.1371/journal.pone.0078832. eCollection 2013. PubMed PMID: 24205328; PubMed Central PMCID: PMC3799749.

3: Pezuk JA, Brassesco MS, Morales AG, de Oliveira JC, de Paula Queiroz RG, Machado HR, Carlotti CG Jr, Neder L, Scrideli CA, Tone LG. Polo-like kinase 1 inhibition causes decreased proliferation by cell cycle arrest, leading to cell death in glioblastoma. Cancer Gene Ther. 2013 Sep;20(9):499-506. doi: 10.1038/cgt.2013.46. Epub 2013 Jul 26. PubMed PMID: 23887645.

4: Brassesco MS, Pezuk JA, Morales AG, de Oliveira JC, Roberto GM, da Silva GN, Francisco de Oliveira H, Scrideli CA, Tone LG. In vitro targeting of Polo-like kinase 1 in bladder carcinoma: comparative effects of four potent inhibitors. Cancer Biol Ther. 2013 Jul;14(7):648-57. doi: 10.4161/cbt.25087. Epub 2013 May 31. PubMed PMID: 23792639; PubMed Central PMCID: PMC3742494.

5: Vazquez-Martin A, Corominas-Faja B, Oliveras-Ferraros C, Cufí S, Dalla Venezia N, Menendez JA. Serine79-phosphorylated acetyl-CoA carboxylase, a downstream target of AMPK, localizes to the mitotic spindle poles and the cytokinesis furrow. Cell Cycle. 2013 May 15;12(10):1639-41. doi: 10.4161/cc.24700. Epub 2013 Apr 19. PubMed PMID: 23603990; PubMed Central PMCID: PMC3680544.

6: Vazquez-Martin A, Cufí S, Oliveras-Ferraros C, Menendez JA. Raptor, a positive regulatory subunit of mTOR complex 1, is a novel phosphoprotein of the rDNA transcription machinery in nucleoli and chromosomal nucleolus organizer regions (NORs). Cell Cycle. 2011 Sep 15;10(18):3140-52. Epub 2011 Sep 15. PubMed PMID: 21900751.

7: Spaniol K, Boos J, Lanvers-Kaminsky C. An in-vitro evaluation of the polo-like kinase inhibitor GW843682X against paediatric malignancies. Anticancer Drugs. 2011 Jul;22(6):531-42. doi: 10.1097/CAD.0b013e3283454526. PubMed PMID: 21637161.

8: Liu XS, Liu X. Targeting Plk1 in cutaneous T-cell lymphomas (CTCLs). Cell Cycle. 2011 May 15;10(10):1523. Epub 2011 May 15. PubMed PMID: 21478668.

9: Vazquez-Martin A, Oliveras-Ferraros C, Cufí S, Menendez JA. Polo-like kinase 1 regulates activation of AMP-activated protein kinase (AMPK) at the mitotic apparatus. Cell Cycle. 2011 Apr 15;10(8):1295-302. Epub 2011 Apr 15. PubMed PMID: 21474997.

10: Nihal M, Stutz N, Schmit T, Ahmad N, Wood GS. Polo-like kinase 1 (Plk1) is expressed by cutaneous T-cell lymphomas (CTCLs), and its downregulation promotes cell cycle arrest and apoptosis. Cell Cycle. 2011 Apr 15;10(8):1303-11. Epub 2011 Apr 15. PubMed PMID: 21436619.

11: Li Z, Umeyama T, Li Z, Wang CC. Polo-like kinase guides cytokinesis in Trypanosoma brucei through an indirect means. Eukaryot Cell. 2010 May;9(5):705-16. doi: 10.1128/EC.00330-09. Epub 2010 Mar 12. PubMed PMID: 20228202; PubMed Central PMCID: PMC2863957.

12: Ikezoe T, Yang J, Nishioka C, Takezaki Y, Tasaka T, Togitani K, Koeffler HP, Yokoyama A. A novel treatment strategy targeting polo-like kinase 1 in hematological malignancies. Leukemia. 2009 Sep;23(9):1564-76. doi: 10.1038/leu.2009.94. Epub 2009 May 7. PubMed PMID: 19421227.

13: Didier C, Cavelier C, Quaranta M, Demur C, Ducommun B. Evaluation of Polo-like Kinase 1 inhibition on the G2/M checkpoint in Acute Myelocytic Leukaemia. Eur J Pharmacol. 2008 Sep 4;591(1-3):102-5. doi: 10.1016/j.ejphar.2008.06.062. Epub 2008 Jun 19. PubMed PMID: 18616938.

14: Lansing TJ, McConnell RT, Duckett DR, Spehar GM, Knick VB, Hassler DF, Noro N, Furuta M, Emmitte KA, Gilmer TM, Mook RA Jr, Cheung M. In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1. Mol Cancer Ther. 2007 Feb;6(2):450-9. Epub 2007 Jan 31. PubMed PMID: 17267659.

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