WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H130064
CAS#: 2272904-53-5
Description: Zasocitinib, also commonly known as NDI-034858 and TAK-279, is an allosteric TYK2 inhibitor for anti-inflammatory applications. Phase 2b trials have been undergone for use of Zasocitinib as a treatment for moderate-to-severe plaque psoriasis in adults.
Hodoodo Cat#: H130064
Name: Zasocitinib
CAS#: 2272904-53-5
Chemical Formula: C23H24N8O3
Exact Mass: 460.20
Molecular Weight: 460.500
Elemental Analysis: C, 59.99; H, 5.25; N, 24.33; O, 10.42
Synonym: Zasocitinib; NDI-034858; NDI034858; NDI 034858; TAK-279; TAK 279; TAK279;
IUPAC/Chemical Name: N-[(1R,2R)-2-methoxycyclobutyl]-7-(methylamino)-5-[(2-oxo[1(2H),2'-bipyridin]-3-yl)amino]-pyrazolo[1,5-a]pyrimidine-3-carboxamide
InChi Key: BWINBHTTZLVXGT-NVXWUHKLSA-N
InChi Code: InChI=1S/C23H24N8O3/c1-24-20-12-18(27-16-6-5-11-30(23(16)33)19-7-3-4-10-25-19)29-21-14(13-26-31(20)21)22(32)28-15-8-9-17(15)34-2/h3-7,10-13,15,17,24H,8-9H2,1-2H3,(H,27,29)(H,28,32)/t15-,17-/m1/s1
SMILES Code: O=C(C1=C2N=C(NC3=CC=CN(C4=NC=CC=C4)C3=O)C=C(NC)N2N=C1)N[C@H]5[C@H](OC)CC5
Appearance: To be determined
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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: Cytokines, such as those in the interleukin (IL)-23/IL-17 axis, play an important role in the pathogenesis of psoriasis. Janus kinase, along with STAT, regulate intracellular signaling of key cytokines involved in the (IL)-23/IL-17 axis. TYK2 inhibition leads to the suppression of these signals.
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 460.50 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: | |
In vitro protocol: | |
In vivo protocol: |
Loo WJ, Turchin I, Prajapati VH, Gooderham MJ, Grewal P, Hong CH, Sauder M, Vender RB, Maari C, Papp KA. Clinical Implications of Targeting the JAK-STAT Pathway in Psoriatic Disease: Emphasis on the TYK2 Pathway. J Cutan Med Surg. 2023 Jan-Feb;27(1_suppl):3S-24S. doi: 10.1177/12034754221141680. Epub 2022 Dec 15. PMID: 36519621.
https://www.nimbustx.com/2022/11/30/nimbus-therapeutics-announces-positive-topline-results-for-phase-2b-clinical-trial-of-allosteric-tyk2-inhibitor-in-psoriasis/
https://clinicaltrials.gov/ct2/show/NCT04999839