RWJ-67657 | CAS#215303-72-3 | p38 MAPK inhibitor |

RWJ-67657
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 510234

CAS#: 215303-72-3

Description: RWJ-67657 is a potent p38 MAPK inhibitor. RWJ-67657 displays cardioprotective and anti-inflammatory activity in vivo.

Chemical Structure

RWJ-67657

CAS# 215303-72-3

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 510234
Name: RWJ-67657
CAS#: 215303-72-3
Chemical Formula: C27H24FN3O
Exact Mass: 425.19
Molecular Weight: 425.500
Elemental Analysis: C, 76.21; H, 5.69; F, 4.46; N, 9.88; O, 3.76

Price and Availability

Size	Price	Availability
10mg	USD 300	2 Weeks
50mg	USD 950	2 Weeks
100mg	USD 1650	2 Weeks
200mg	USD 2850	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: RWJ67657; RWJ-67657; RWJ 67657

IUPAC/Chemical Name: 4-(4-(4-fluorophenyl)-1-(3-phenylpropyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl)but-3-yn-1-ol

InChi Key: QSUSKMBNZQHHPA-UHFFFAOYSA-N

InChi Code: InChI=1S/C27H24FN3O/c28-24-13-11-22(12-14-24)26-27(23-15-17-29-18-16-23)31(25(30-26)10-4-5-20-32)19-6-9-21-7-2-1-3-8-21/h1-3,7-8,11-18,32H,5-6,9,19-20H2

SMILES Code: OCCC#CC1=NC(C2=CC=C(F)C=C2)=C(C3=CC=NC=C3)N1CCCC4=CC=CC=C4

Appearance: white 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 and ethanol

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:	RWJ-67657 is a selective p38α and p38β inhibitor (IC50s = 1 and 11 μM respectively) that displays no activity at p38γ, p38δ and a range of other kinases. RWJ-67657 potently inhibits TNF-α and IL-1β release (IC50s = 3 and 11 nM respectively) and suppresses HIV-1 replication in T cells in vitro.
In vitro activity:	RWJ-67657 effectively inhibited HIV-1 replication in both T-cell and monocyte cell lines, irrespective of the coreceptor used by the virus for entry into the cell. RWJ-67657 effectively suppressed both reverse transcriptase and protease resistant escape mutant viruses. Reference: AIDS. 2004 Mar 26;18(5):739-48. https://pubmed.ncbi.nlm.nih.gov/15075508/
In vivo activity:	The pharmacological inhibition of p38 with RWJ-67657 led to a decrease in chemoresistant cancer tumor growth in xenograft animal models. This suggests that RWJ-67657 has potential therapeutic relevance in reversing epithelial-to-mesenchymal transition in advanced tumor phenotypes and overcoming drug resistance in breast cancer. Reference: Int J Oncol. 2013 Apr;42(4):1139-50. https://pubmed.ncbi.nlm.nih.gov/23403951/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	42.6	100.00
	Ethanol	42.6	100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 425.50 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. Huang KW, Wang IH, Fu P, Krum H, Bach LA, Wang BH. Insulin-like growth factor-1 directly affects cardiac cellular remodelling via distinct pathways. Int J Cardiol Heart Vasc. 2021 Aug 2;36:100852. doi: 10.1016/j.ijcha.2021.100852. PMID: 34401470; PMCID: PMC8349770. 2. Muthumani K, Wadsworth SA, Dayes NS, Hwang DS, Choo AY, Abeysinghe HR, Siekierka JJ, Weiner DB. Suppression of HIV-1 viral replication and cellular pathogenesis by a novel p38/JNK kinase inhibitor. AIDS. 2004 Mar 26;18(5):739-48. doi: 10.1097/00002030-200403260-00004. PMID: 15075508. 3. Antoon JW, Nitzchke AM, Martin EC, Rhodes LV, Nam S, Wadsworth S, Salvo VA, Elliott S, Collins-Burow B, Nephew KP, Burow ME. Inhibition of p38 mitogen-activated protein kinase alters microRNA expression and reverses epithelial-to-mesenchymal transition. Int J Oncol. 2013 Apr;42(4):1139-50. doi: 10.3892/ijo.2013.1814. Epub 2013 Feb 8. PMID: 23403951; PMCID: PMC3622654. 4. Kompa AR, See F, Lewis DA, Adrahtas A, Cantwell DM, Wang BH, Krum H. Long-term but not short-term p38 mitogen-activated protein kinase inhibition improves cardiac function and reduces cardiac remodeling post-myocardial infarction. J Pharmacol Exp Ther. 2008 Jun;325(3):741-50. doi: 10.1124/jpet.107.133546. Epub 2008 Mar 11. PMID: 18334667.
In vitro protocol:	1. Huang KW, Wang IH, Fu P, Krum H, Bach LA, Wang BH. Insulin-like growth factor-1 directly affects cardiac cellular remodelling via distinct pathways. Int J Cardiol Heart Vasc. 2021 Aug 2;36:100852. doi: 10.1016/j.ijcha.2021.100852. PMID: 34401470; PMCID: PMC8349770. 2. Muthumani K, Wadsworth SA, Dayes NS, Hwang DS, Choo AY, Abeysinghe HR, Siekierka JJ, Weiner DB. Suppression of HIV-1 viral replication and cellular pathogenesis by a novel p38/JNK kinase inhibitor. AIDS. 2004 Mar 26;18(5):739-48. doi: 10.1097/00002030-200403260-00004. PMID: 15075508.
In vivo protocol:	1. Antoon JW, Nitzchke AM, Martin EC, Rhodes LV, Nam S, Wadsworth S, Salvo VA, Elliott S, Collins-Burow B, Nephew KP, Burow ME. Inhibition of p38 mitogen-activated protein kinase alters microRNA expression and reverses epithelial-to-mesenchymal transition. Int J Oncol. 2013 Apr;42(4):1139-50. doi: 10.3892/ijo.2013.1814. Epub 2013 Feb 8. PMID: 23403951; PMCID: PMC3622654. 2. Kompa AR, See F, Lewis DA, Adrahtas A, Cantwell DM, Wang BH, Krum H. Long-term but not short-term p38 mitogen-activated protein kinase inhibition improves cardiac function and reduces cardiac remodeling post-myocardial infarction. J Pharmacol Exp Ther. 2008 Jun;325(3):741-50. doi: 10.1124/jpet.107.133546. Epub 2008 Mar 11. PMID: 18334667.

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1: Westra J, Kułdo JM, van Rijswijk MH, Molema G, Limburg PC. Chemokine production and E-selectin expression in activated endothelial cells are inhibited by p38 MAPK (mitogen activated protein kinase) inhibitor RWJ 67657. Int Immunopharmacol. 2005 Jul;5(7-8):1259-69. Epub 2005 Apr 26. PubMed PMID: 15914330.

2: Westra J, Limburg PC, de Boer P, van Rijswijk MH. Effects of RWJ 67657, a p38 mitogen activated protein kinase (MAPK) inhibitor, on the production of inflammatory mediators by rheumatoid synovial fibroblasts. Ann Rheum Dis. 2004 Nov;63(11):1453-9. PubMed PMID: 15479895; PubMed Central PMCID: PMC1754789.

3: Westra J, Doornbos-van der Meer B, de Boer P, van Leeuwen MA, van Rijswijk MH, Limburg PC. Strong inhibition of TNF-alpha production and inhibition of IL-8 and COX-2 mRNA expression in monocyte-derived macrophages by RWJ 67657, a p38 mitogen-activated protein kinase (MAPK) inhibitor. Arthritis Res Ther. 2004;6(4):R384-92. Epub 2004 Jun 21. PubMed PMID: 15225374; PubMed Central PMCID: PMC464924.

4: Parasrampuria DA, de Boer P, Desai-Krieger D, Chow AT, Jones CR. Single-dose pharmacokinetics and pharmacodynamics of RWJ 67657, a specific p38 mitogen-activated protein kinase inhibitor: a first-in-human study. J Clin Pharmacol. 2003 Apr;43(4):406-13. PubMed PMID: 12723461.

5: Faas MM, Moes H, Fijen JW, Muller Kobold AC, Tulleken JE, Zijlstra JG. Monocyte intracellular cytokine production during human endotoxaemia with or without a second in vitro LPS challenge: effect of RWJ-67657, a p38 MAP-kinase inhibitor, on LPS-hyporesponsiveness. Clin Exp Immunol. 2002 Feb;127(2):337-43. PubMed PMID: 11876759; PubMed Central PMCID: PMC1906333.

6: Fijen JW, Zijlstra JG, De Boer P, Spanjersberg R, Tervaert JW, Van Der Werf TS, Ligtenberg JJ, Tulleken JE. Suppression of the clinical and cytokine response to endotoxin by RWJ-67657, a p38 mitogen-activated protein-kinase inhibitor, in healthy human volunteers. Clin Exp Immunol. 2001 Apr;124(1):16-20. PubMed PMID: 11359438; PubMed Central PMCID: PMC1906020.

7: Wadsworth SA, Cavender DE, Beers SA, Lalan P, Schafer PH, Malloy EA, Wu W, Fahmy B, Olini GC, Davis JE, Pellegrino-Gensey JL, Wachter MP, Siekierka JJ. RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase. J Pharmacol Exp Ther. 1999 Nov;291(2):680-7. PubMed PMID: 10525088.

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