Itacitinib

Itacitinib, also known as INCB39110 or INCB039110, is a potent, selective and orally bioavailable inhibitor of JAK1 (Janus-associated kinase 1) with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2 (IC50 for JAK1, 2, 3, and TYK2 are 2, 63, >2000, and 795 nM, respectively). It has potential antineoplastic activity and is currently in Phase II clinical trials for the treatment of myelofibrosis, rheumatoid arthritis and plaque psoriasis. Janus kinases (JAKs) are a family of four enzymes; JAK1, JAK2, JAK3 and tyrosine kinase 2 (TYK2) that are critical in cytokine signalling and are strongly linked to both cancer and inflammatory diseases. For example, constitutive activation of the inflammation-related IL-6/JAK/STAT3 signaling pathway has been reported in pancreatic tumors and has been suggested to be a poor prognostic factor for overall survival in patients with advanced disease.


Cat. No.: EX-A1674	Purity: >98%

For research only, Do not use for Human!

Size	Unit Price (US$)	Stock
100mg	765	In-stock
250mg	1065	In-stock
500mg	1565	In-stock
1g	2165	In-stock
5g	6350	In-stock
10g	9850	In-stock

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Synonyms	INCB039110
CAS No.	1334298-90-6
Purity	>98%
Formula	C26H23F4N9O
Mol Weight	553.5141
Appearance	solid powder
Solubility	Soluble in DMSO
Shelf Life	>2 years if stored properly
Storage	Powder -20℃ 2 years; In solvent -20℃ 1 month;
Shipping	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.

Reference:	[1]. Mascarenhas JO, et al. Primary analysis of a phase II open-label trial of INCB039110, a selective JAK1 inhibitor, in patients with myelofibrosis. Haematologica. 2017 Feb;102(2):327-335. PMID: 27789678. [2]. Bissonnette R, et al. A randomized, double-blind, placebo-controlled, dose-escalation study of the safety and efficacy of INCB039110, an oral janus kinase 1 inhibitor, in patients with stable, chronic plaque psoriasis. J Dermatolog Treat. 2016 Jan 14;1-7. PMID: 26769332.
CoA	CoA of Itacitinib

Smiles:	FC1=C(C=CN=C1C(F)(F)F)C(=O)N1CCC(CC1)N1CC(CC#N)(C1)N1C=C(C=N1)C1=C2C=CNC2=NC=N1


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