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Izencitinib

Catalog No. T35898 CAS 2051918-33-1

Izencitinib (TD-1473) is an orally active, gut-restricted JAK inhibitor with non-selective properties. It is primarily employed in the investigation of ulcerative colitis [1].

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Izencitinib, CAS 2051918-33-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 88.00
5 mg	In stock	$ 213.00
10 mg	In stock	$ 347.00
25 mg	In stock	$ 695.00
50 mg	In stock	$ 1,090.00
100 mg	In stock	$ 1,790.00
1 mL * 10 mM (in DMSO)	In stock	$ 235.00

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Purity: 99.82%

ee: 100%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Izencitinib (TD-1473) is an orally active, gut-restricted JAK inhibitor with non-selective properties. It is primarily employed in the investigation of ulcerative colitis [1].
In vitro	Izencitinib (TD-1473) inhibits cytokine-evoked STAT phosphorylation in human peripheral blood mononuclear cells (PBMCs) and in a human colonic epithelial cell line (pIC50 ≥ 6.7)[1].Izencitinib (TD-1473) is a potent JAK1, JAK2, JAK3, and TYK2 inhibitor at the human JAK kinase domains (pKi values of 10.0, 10.0, 8.8, and 9.5, respectively)[1].
In vivo	Izencitinib (TD-1473, 1 mg/kg BID) preserves body weight and reduced occult blood scores in a mouse oxazolone colitis model[1].

Molecular Weight	402.5
Formula	C22H26N8
CAS No.	2051918-33-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (124.22 mM), Sonication is recommended.

References and Literature

1. Kevin S Currie, et al. Small-molecule agents for the treatment of inflammatory bowel disease. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2034-2041. 2. William J Sandborn, et al. Development of Gut-Selective Pan-Janus Kinase Inhibitor TD-1473 for Ulcerative Colitis: A Translational Medicine Programme. J Crohns Colitis. 2020 Sep 16;14(9):1202-1213. 3. D. Beattie, et al. TD-1473, a novel, potent, and orally administered, GI-targeted, pan-Janus kinase (JAK) inhibitor. Journal of Crohn’s and Colitis, Volume 10, Issue suppl_1, March 2016, Page S123.

Dose Conversion

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
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The answer of 19.713 mg appears in the Mass box

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An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Izencitinib 2051918-33-1 inhibitor inhibit

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