Itacitinib (INCB-039110)

Alias: Itacitinib;INCB039110; INCB-039110; INCB 039110; INCB39110; INCB 39110; INCB-39110
Cat No.:V0065 Purity: ≥98%
Itacitinib (also known as INCB39110) 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).
Itacitinib (INCB-039110) Chemical Structure CAS No.: 1334298-90-6
Product category: JAK
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Itacitinib (INCB-039110):

  • Itacitinib adipate (INCB 39110 adipate)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Itacitinib (also known as INCB39110) 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.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Itacitinib (INCB039110) is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2. Myelofibrosis research employs itacitinib [1].
ln Vivo
Itacitinib is able to inhibit tumor growth in human pancreatic xenograft models in mice at clinically relevant doses, both as monotherapy and in combination with cytotoxic agents such as gemcitabine.
Animal Protocol
N/A
Human pancreatic xenograft models in mice
References
[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.
[2]. Alain Lescoat, et al. Combined Anti-Fibrotic and Anti-Inflammatory Properties of JAK-inhibitors on Macrophages in Vitro and in Vivo: Perspectives for Scleroderma-Associated Interstitial Lung Disease. Biochem Pharmacol. 2020 Jun 17;114103.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C26H23F4N9O
Molecular Weight
553.51
CAS #
1334298-90-6
SMILES
N#CCC1(N2N=CC(C3=C4C(NC=C4)=NC=N3)=C2)CN(C5CCN(C(C6=C(F)C(C(F)(F)F)=NC=C6)=O)CC5)C1
Chemical Name
2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(1-(3-fluoro-2-(trifluoromethyl)isonicotinoyl) piperidin-4-yl)azetidin-3-yl)acetonitrile
Synonyms
Itacitinib;INCB039110; INCB-039110; INCB 039110; INCB39110; INCB 39110; INCB-39110
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:>90 mg/mL
Water:<1 mg/mL
Ethanol:>90 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.8067 mL 9.0333 mL 18.0665 mL
5 mM 0.3613 mL 1.8067 mL 3.6133 mL
10 mM 0.1807 mL 0.9033 mL 1.8067 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Itacitinib

    Treatment effects on total symptom score (TSS).2017 Feb;102(2):327-335.

  • Itacitinib

    Treatment effects on spleen volume.2017 Feb;102(2):327-335.

  • Itacitinib

    Mean hemoglobin level and platelet count over time by dose cohort.2017 Feb;102(2):327-335.

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