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MedKoo Cat#: 406121 | Name: WHI-P154
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Description:

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

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).

Chemical Structure

WHI-P154
WHI-P154
CAS#211555-04-3

Theoretical Analysis

MedKoo Cat#: 406121

Name: WHI-P154

CAS#: 211555-04-3

Chemical Formula: C16H14BrN3O3

Exact Mass: 375.0219

Molecular Weight: 376.20

Elemental Analysis: C, 51.08; H, 3.75; Br, 21.24; N, 11.17; O, 12.76

Price and Availability

Size Price Availability Quantity
5mg USD 90.00 Ready to ship
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to ship
500mg USD 2,650.00 Ready to ship
1g USD 4,250.00 Ready to ship
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Related CAS #
No Data
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
More Info
        

Preparing Stock Solutions

The following data is based on the product molecular weight 376.20 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: Le K, Vollenweider J, Han J, Staudinger N, Stenson M, Bayraktar L, Wellik LE, Maurer MJ, McPhail ED, Witzig TE, Gupta M. Dependence of peripheral T-cell lymphoma on constitutively activated JAK3: Implication for JAK3 inhibition as a therapeutic approach. Hematol Oncol. 2024 Jan;42(1):e3233. doi: 10.1002/hon.3233. Epub 2023 Oct 24. PMID: 37876297. 2: Lee JY, Kim SH, Lee SH, Kim HR, Min HK. Effect of Janus kinase inhibitors on T cell responses to herpes zoster in rheumatoid arthritis patients. Clin Exp Rheumatol. 2023 May;41(5):1077-1087. doi: 10.55563/clinexprheumatol/xzgaoy. Epub 2022 Aug 31. PMID: 36062760. 3: Yan B, Liu P, Yi X, Li J, Liu N, Zhu W, Kuang Y, Chen X, Peng C. Topical VX-509 attenuates psoriatic inflammation through the STAT3/FABP5 pathway in keratinocytes. Pharmacol Res. 2022 Aug;182:106318. doi: 10.1016/j.phrs.2022.106318. Epub 2022 Jun 18. PMID: 35728766. 4: Liu Z, Wang Y, Shi J, Chen S, Xu L, Li F, Dong N. IL-21 promotes osteoblastic differentiation of human valvular interstitial cells through the JAK3/STAT3 pathway. Int J Med Sci. 2020 Oct 20;17(18):3065-3072. doi: 10.7150/ijms.49533. PMID: 33173427; PMCID: PMC7646116. 5: Meng Y, Gao C, Clawson DK, Atwell S, Russell M, Vieth M, Roux B. Predicting the Conformational Variability of Abl Tyrosine Kinase using Molecular Dynamics Simulations and Markov State Models. J Chem Theory Comput. 2018 May 8;14(5):2721-2732. doi: 10.1021/acs.jctc.7b01170. Epub 2018 Apr 3. PMID: 29474075; PMCID: PMC6317529. 6: Bhavsar SK, Singh Y, Sharma P, Khairnar V, Hosseinzadeh Z, Zhang S, Palmada M, Sabolic I, Koepsell H, Lang KS, Lang PA, Lang F. Expression of JAK3 Sensitive Na+ Coupled Glucose Carrier SGLT1 in Activated Cytotoxic T Lymphocytes. Cell Physiol Biochem. 2016;39(3):1209-28. doi: 10.1159/000447827. Epub 2016 Sep 5. PMID: 27595398. 7: Yan J, Zhang B, Hosseinzadeh Z, Lang F. Down-Regulation of Store-Operated Ca2+ Entry and Na+ Ca2+ Exchange in MCF-7 Breast Cancer Cells by Pharmacological JAK3 Inhibition. Cell Physiol Biochem. 2016;38(4):1643-51. doi: 10.1159/000443104. Epub 2016 Apr 28. PMID: 27119652. 8: Fezai M, Warsi J, Lang F. Regulation of the Na+,Cl- Coupled Creatine Transporter CreaT (SLC6A8) by the Janus Kinase JAK3. Neurosignals. 2015;23(1):11-9. doi: 10.1159/000442600. Epub 2015 Dec 14. PMID: 26666525. 9: Warsi J, Abousaab A, Fezai M, Elvira B, Lang F. Regulation of Voltage Gated K+ Channel KCNE1/KCNQ1 by the Janus Kinase JAK3. Cell Physiol Biochem. 2015;37(6):2476-85. doi: 10.1159/000438600. Epub 2015 Dec 14. PMID: 26666518. 10: Yan J, Schmid E, Hosseinzadeh Z, Honisch S, Shumilina E, Fuchs J, Lang F. Impact of Janus Kinase 3 on Cellular Ca Release, Store Operated Ca(2+) Entry and Na(+)/Ca(2+) Exchanger Activity in Dendritic Cells. Cell Physiol Biochem. 2015;36(6):2287-98. doi: 10.1159/000430192. Epub 2015 Jul 24. PMID: 26279433. 11: Hosseinzadeh Z, Honisch S, Schmid E, Jilani K, Szteyn K, Bhavsar S, Singh Y, Palmada M, Umbach AT, Shumilina E, Lang F. The Role of Janus Kinase 3 in the Regulation of Na⁺/K⁺ ATPase under Energy Depletion. Cell Physiol Biochem. 2015;36(2):727-40. doi: 10.1159/000430133. Epub 2015 May 22. PMID: 26021261. 12: Kakutani Y, Shioi A, Shoji T, Okazaki H, Koyama H, Emoto M, Inaba M. Oncostatin M Promotes Osteoblastic Differentiation of Human Vascular Smooth Muscle Cells Through JAK3-STAT3 Pathway. J Cell Biochem. 2015 Jul;116(7):1325-33. doi: 10.1002/jcb.25088. PMID: 25735629. 13: Wang YJ, Zhang YK, Kathawala RJ, Chen ZS. Repositioning of Tyrosine Kinase Inhibitors as Antagonists of ATP-Binding Cassette Transporters in Anticancer Drug Resistance. Cancers (Basel). 2014 Sep 29;6(4):1925-52. doi: 10.3390/cancers6041925. PMID: 25268163; PMCID: PMC4276951. 14: Warsi J, Luo D, Elvira B, Jilani K, Shumilina E, Hosseinzadeh Z, Lang F. Upregulation of excitatory amino acid transporters by coexpression of Janus kinase 3. J Membr Biol. 2014 Aug;247(8):713-20. doi: 10.1007/s00232-014-9695-3. Epub 2014 Jun 14. PMID: 24928228. 15: 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 Aug;105(8):1071-8. doi: 10.1111/cas.12462. Epub 2014 Aug 21. PMID: 24903205; PMCID: PMC4317847. 16: Warsi J, Elvira B, Hosseinzadeh Z, Shumilina E, Lang F. Downregulation of chloride channel ClC-2 by Janus kinase 3. J Membr Biol. 2014 May;247(5):387-93. doi: 10.1007/s00232-014-9645-0. Epub 2014 Mar 11. PMID: 24615260. 17: Warsi J, Hosseinzadeh Z, Dong L, Pakladok T, Umbach AT, Bhavsar SK, Shumilina E, Lang F. Effect of Janus kinase 3 on the peptide transporters PEPT1 and PEPT2. J Membr Biol. 2013 Dec;246(12):885-92. doi: 10.1007/s00232-013-9582-3. Epub 2013 Aug 10. PMID: 23934551. 18: Wang G, Qian P, Xu Z, Zhang J, Wang Y, Cheng S, Cai W, Qian G, Wang C, Decoster MA. Regulatory effects of the JAK3/STAT1 pathway on the release of secreted phospholipase A₂-IIA in microvascular endothelial cells of the injured brain. J Neuroinflammation. 2012 Jul 12;9:170. doi: 10.1186/1742-2094-9-170. PMID: 22788969; PMCID: PMC3409030. 19: Jang YN, Lee IJ, Park MC, Baik EJ. Role of JAK3 in myogenic differentiation. Cell Signal. 2012 Mar;24(3):742-9. doi: 10.1016/j.cellsig.2011.11.009. Epub 2011 Nov 18. PMID: 22120524. 20: Wang YW, Tu PH, Lin KT, Lin SC, Ko JY, Jou YS. Identification of oncogenic point mutations and hyperphosphorylation of anaplastic lymphoma kinase in lung cancer. Neoplasia. 2011 Aug;13(8):704-15. doi: 10.1593/neo.11222. PMID: 21847362; PMCID: PMC3156661.

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TRC-160334

TRC-160334