WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406122
Description: WP1066 is a Stat3 inhibitor and JAK2 inhibitor. WP1066 is also a novel analogue of the JAK2 inhibitor AG490, in JAK2 V617F-positive erythroleukemia HEL cells and in blood cells from patients with polycythemia vera. WP1066 significantly inhibited JAK2 and its downstream signal transducer and activator of transcription-3, signal transducer and activator of transcription-5, and extracellular signal-regulated kinase-1/2 pathways in a dose- and time-dependent manner. WP1066 is active both in vitro and ex vivo and should be further developed for the treatment of neoplasms expressing the JAK2 V617F mutation.
MedKoo Cat#: 406122
Chemical Formula: C17H14BrN3O
Exact Mass: 355.03202
Molecular Weight: 356.22
Elemental Analysis: C, 57.32; H, 3.96; Br, 22.43; N, 11.80; O, 4.49
Synonym: WP1066; WP 1066; WP-1066
IUPAC/Chemical Name: (S,E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide
InChi Key: VFUAJMPDXIRPKO-LQELWAHVSA-N
InChi Code: InChI=1S/C17H14BrN3O/c1-12(13-6-3-2-4-7-13)20-17(22)14(11-19)10-15-8-5-9-16(18)21-15/h2-10,12H,1H3,(H,20,22)/b14-10+/t12-/m0/s1
SMILES Code: O=C(N[C@H](C1=CC=CC=C1)C)/C(C#N)=C/C2=NC(Br)=CC=C2
Appearance: White to off-white crystalline 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
The following data is based on the product molecular weight 356.22 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|
1: Hatiboglu MA, Kong LY, Wei J, Wang Y, McEnery KA, Fuller GN, Qiao W, Davies MA, Priebe W, Heimberger AB. The tumor microenvironment expression of p-STAT3 influences the efficacy of cyclophosphamide with WP1066 in murine melanoma models. Int J Cancer. 2012 Jul 1;131(1):8-17. doi: 10.1002/ijc.26307. Epub 2011 Aug 24. PubMed PMID: 21792892; PubMed Central PMCID: PMC3319790.
2: Horiguchi A, Asano T, Kuroda K, Sato A, Asakuma J, Ito K, Hayakawa M, Sumitomo M, Asano T. STAT3 inhibitor WP1066 as a novel therapeutic agent for renal cell carcinoma. Br J Cancer. 2010 May 25;102(11):1592-9. doi: 10.1038/sj.bjc.6605691. Epub 2010 May 11. PubMed PMID: 20461084; PubMed Central PMCID: PMC2883159.
3: Verstovsek S, Manshouri T, QuintÃ¡s-Cardama A, Harris D, Cortes J, Giles FJ, Kantarjian H, Priebe W, Estrov Z. WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation. Clin Cancer Res. 2008 Feb 1;14(3):788-96. doi: 10.1158/1078-0432.CCR-07-0524. PubMed PMID: 18245540.
4: Ferrajoli A, Faderl S, Van Q, Koch P, Harris D, Liu Z, Hazan-Halevy I, Wang Y, Kantarjian HM, Priebe W, Estrov Z. WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells. Cancer Res. 2007 Dec 1;67(23):11291-9. PubMed PMID: 18056455.