WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406121
Description: WHI-P154 is a JAK3 inhibitor with IC50 = 1.8 microM. WHI-P154 displays no activity at JAK1 or JAK2. WHI-P154 also Inhibits STAT1 activation, iNOS expression and NO production in macrophages in vitro . Also inhibits other common kinases including EGFR (IC50 = 4 nM), Src, Abl, VEGFR, MAPK and PI 3-K and induces apoptosis in human glioblastoma cell lines (IC50 = 158 microM).
MedKoo Cat#: 406121
Chemical Formula: C16H14BrN3O3
Exact Mass: 375.02185
Molecular Weight: 376.2
Elemental Analysis: C, 51.08; H, 3.75; Br, 21.24; N, 11.17; O, 12.76
Synonym: WHIP154; WHI P154; WHIP 154; Janex1.
IUPAC/Chemical Name: 2-Bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]phenol
InChi Key: CBIAKDAYHRWZCU-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H14BrN3O3/c1-22-14-6-10-12(7-15(14)23-2)18-8-19-16(10)20-9-3-4-13(21)11(17)5-9/h3-8,21H,1-2H3,(H,18,19,20)
SMILES Code: OC1=CC=C(NC2=C3C=C(OC)C(OC)=CC3=NC=N2)C=C1Br
Appearance: White to grey 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: >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 376.2 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: Zhang H, Zhang YK, Wang YJ, Kathawala RJ, Patel A, Zhu H, Sodani K, Talele TT, Ambudkar SV, Chen ZS, Fu LW. WHI-P154 Enhances the Chemotherapeutic Effect of Anticancer Agents in ABCG2-overexpressing Cells. Cancer Sci. 2014 Jun 5. doi: 10.1111/cas.12462. [Epub ahead of print] PubMed PMID: 24903205.
2: Sareila O, Korhonen R, KÃ¤rpÃ¤nniemi O, Nieminen R, Kankaanranta H, Moilanen E. Janus kinase 3 inhibitor WHI-P154 in macrophages activated by bacterial endotoxin: differential effects on the expression of iNOS, COX-2 and TNF-alpha. Int Immunopharmacol. 2008 Jan;8(1):100-8. Epub 2007 Nov 20. PubMed PMID: 18068105.
3: Sareila O, Korhonen R, KÃ¤rpÃ¤nniemi O, Nieminen R, Kankaanranta H, Moilanen E. JAK inhibitors AG-490 and WHI-P154 decrease IFN-gamma-induced iNOS expression and NO production in macrophages. Mediators Inflamm. 2006;2006(2):16161. PubMed PMID: 16883061; PubMed Central PMCID: PMC1592588.
4: Richards GR, Smith AJ, Cuddon P, Ma QP, Leveridge M, Kerby J, Roderick HL, Bootman MD, Simpson PB. The JAK3 inhibitor WHI-P154 prevents PDGF-evoked process outgrowth in human neural precursor cells. J Neurochem. 2006 Apr;97(1):201-10. Epub 2006 Mar 3. PubMed PMID: 16515549.
5: Linwong W, Hirasawa N, Aoyama S, Hamada H, Saito T, Ohuchi K. Inhibition of the antigen-induced activation of rodent mast cells by putative Janus kinase 3 inhibitors WHI-P131 and WHI-P154 in a Janus kinase 3-independent manner. Br J Pharmacol. 2005 Jul;145(6):818-28. PubMed PMID: 15852029; PubMed Central PMCID: PMC1576194.
6: Narla RK, Liu XP, Klis D, Uckun FM. Inhibition of human glioblastoma cell adhesion and invasion by 4-(4'-hydroxylphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P131) and 4-(3'-bromo-4'-hydroxylphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P154). Clin Cancer Res. 1998 Oct;4(10):2463-71. PubMed PMID: 9796979.