WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H406840
CAS#: 1186653-73-5 (TFA salt)
Description: UK-122, also known as uPA Inhibitor II, is a potent and selective uPA inhibitor (Ki = 20 nM). The IC(50) of UK122 in a cell-free indirect uPA assay is 0.2 micromol/L. UK-122 also showed no or little inhibition of other serine proteases such as thrombin, trypsin, plasmin, and the tissue-type plasminogen activator, indicating its high specificity against uPA. Moreover, UK122 showed little cytotoxicity against CFPAC-1 cells (IC(50) >100 micromol/L) but significantly inhibited the migration and invasion of this pancreatic cancer cell line. UK122 could potentially be developed as a new anticancer agent that prevents the invasion and metastasis of pancreatic cancer.
Hodoodo Cat#: H406840
Name: UK-122 TFA salt
CAS#: 1186653-73-5 (TFA salt)
Chemical Formula: C19H14F3N3O4
Exact Mass: 0.00
Molecular Weight: 405.333
Elemental Analysis: C, 56.30; H, 3.48; F, 14.06; N, 10.37; O, 15.79
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Related CAS #: 1186653-73-5 (TFA salt) 940290-58-4 (free)
Synonym: uPA Inhibitor II, UK-122, UK 122, UK122, UK122 TFA salt, K122 trifloroacetic acid
IUPAC/Chemical Name: (E)-4-((5-oxo-2-phenyloxazol-4(5H)-ylidene)methyl)benzimidamide 2,2,2-trifluoroacetate
InChi Key: KVCIDYPYQWLDKP-KMZJGFRYSA-N
InChi Code: InChI=1S/C17H13N3O2.C2HF3O2/c18-15(19)12-8-6-11(7-9-12)10-14-17(21)22-16(20-14)13-4-2-1-3-5-13;3-2(4,5)1(6)7/h1-10H,(H3,18,19);(H,6,7)/b14-10+;
SMILES Code: N=C(N)C1=CC=C(/C=C2N=C(C3=CC=CC=C3)OC/2=O)C=C1.O=C(O)C(F)(F)F
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: Related CAS# CAS# 940290-58-4 (UK-122 free base) CAS#1186653-73-5 (UK-122 TFA salt)
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The following data is based on the product molecular weight 405.33 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: | |
In vitro protocol: | |
In vivo protocol: |
1: Banyard J, Chung I, Migliozzi M, Phan DT, Wilson AM, Zetter BR, Bielenberg DR. Identification of genes regulating migration and invasion using a new model of metastatic prostate cancer. BMC Cancer. 2014 May 30;14:387. doi: 10.1186/1471-2407-14-387. PubMed PMID: 24885350; PubMed Central PMCID: PMC4046438.
2: Stewart AG, Xia YC, Harris T, Royce S, Hamilton JA, Schuliga M. Plasminogen-stimulated airway smooth muscle cell proliferation is mediated by urokinase and annexin A2, involving plasmin-activated cell signalling. Br J Pharmacol. 2013 Dec;170(7):1421-35. doi: 10.1111/bph.12422. PubMed PMID: 24111848; PubMed Central PMCID: PMC3838688.
3: Cho E, Lee KJ, Seo JW, Byun CJ, Chung SJ, Suh DC, Carmeliet P, Koh JY, Kim JS, Lee JY. Neuroprotection by urokinase plasminogen activator in the hippocampus. Neurobiol Dis. 2012 Apr;46(1):215-24. doi: 10.1016/j.nbd.2012.01.010. Epub 2012 Jan 24. PubMed PMID: 22293605.
4: Zhu M, Gokhale VM, Szabo L, Munoz RM, Baek H, Bashyam S, Hurley LH, Von Hoff DD, Han H. Identification of a novel inhibitor of urokinase-type plasminogen activator. Mol Cancer Ther. 2007 Apr;6(4):1348-56. PubMed PMID: 17431113.