Name: Itacitinib (INCB39110)
Brand: Selleck Chemicals
SKU: S7812
Rating: 5 (11 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	EGFR STAT Pim
Other JAK Inhibitors	BMS-986165 (Deucravacitinib) AZD1480 WP1066 Momelotinib (CYT387) Filgotinib (GLPG0634) AT9283 Gandotinib (LY2784544) Pacritinib (SB1518) TG101209 Cerdulatinib (PRT062070) hydrochloride

Chemical Information, Storage & Stability

Molecular Weight	553.51	Formula	C₂₆H₂₃F₄N₉O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1334298-90-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CN(CCC1N2CC(C2)(CC#N)N3C=C(C=N3)C4=C5C=CNC5=NC=N4)C(=O)C6=C(C(=NC=C6)C(F)(F)F)F

Solubility

In vitro
Batch:

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	6.000mg/ml (10.84mM)	Taking the 1 mL working solution as an example, add 100 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	JAK1
In vitro	INCB039110 is a potent and selective inhibitor of JAK1, with >20 and >200-fold selectivity over JAK2 and JAK3, respectively. The activity against JAK1, 2, 3, and TYK2 are 2, 63, >2000, and 795 nM, respectively.
In vivo	INCB039110 blocks tumour growth in human pancreatic xenograft models in mice at clinically relevant doses, both as monotherapy and in combination with cytotoxic agents.
References	[1] https://pubmed.ncbi.nlm.nih.gov/27774824/ [2] http://cancerres.aacrjournals.org/content/75/15_Supplement/779 [3] https://pubmed.ncbi.nlm.nih.gov/32562787/ [4] https://pubmed.ncbi.nlm.nih.gov/35571736/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05063110	Recruiting	Adults Patients Having Non Severe HLH	Assistance Publique - Hôpitaux de Paris\|Incyte Corporation	May 1 2022	Phase 2
NCT04239989	Active not recruiting	Bronchiolitis Obliterans	M.D. Anderson Cancer Center	April 8 2021	Phase 1
NCT04220632	Terminated	GVHDAcute	Innovent Biologics (Suzhou) Co. Ltd.	June 18 2020	Phase 1\|Phase 2
NCT03978637	Terminated	Bronchiolitis Obliterans Syndrome	Incyte Corporation	February 4 2020	Phase 1\|Phase 2
NCT04070781	Terminated	Steroid Refractory GVHD\|Graft Vs Host Disease	Columbia University\|Incyte Corporation	January 20 2020	Phase 1
NCT03721965	Terminated	Acute Graft-versus-host Disease	Incyte Corporation	December 31 2019	Phase 1\|Phase 2

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Handling Instructions

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Itacitinib (INCB39110) JAK1 Inhibitor

Chemical Structure

Molecular Weight: 553.51