2. Epigenetics
    Stem Cell/Wnt
    Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
    Apoptosis
  3. JAK
    Apoptosis
  4. Ivarmacitinib

Ivarmacitinib  (Synonyms: SHR0302)

Cat. No.: HY-112724 Purity: 99.82%
COA Handling Instructions

Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects.

For research use only. We do not sell to patients.

Ivarmacitinib Chemical Structure

Ivarmacitinib Chemical Structure

CAS No. : 1445987-21-2

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Description

Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects[1][2].

IC50 & Target[1]

JAK1

 

JAK2

 

JAK3

 

Tyk2

 

In Vitro

Ivarmacitinib (SHR0302; 1 nM-10 µM; 48 hours; HSCs) treatment displays an inhibitory effect on the proliferation of HSCs in a concentration-dependent manner[2].
Ivarmacitinib (1 nM-10 µM) exerts an inhibitory effect on the activation, proliferation and migration of HSCs[2].
Ivarmacitinib (1 nM-10 µM; 48 hours; HSCs) treatment induces the apoptosis of HSCs[2].
Ivarmacitinib (1 nM-10 µM; 48 hours; HSCs) treatment significantly increases the activation of caspase-3 and Bax in HSCs, and decreases the expression of Bcl-2. SHR0302 also inhibits the activation of Akt signaling pathway[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: Hepatic stellate cells (HSCs)
Concentration: 1 nM, 10 nM, 100 nM, 1µM, 10 µM
Incubation Time: 48 hours
Result: Displayed an inhibitory effect on the proliferation of HSCs, and that inhibition ocurred in a concentration-dependent manner.

Apoptosis Analysis[2]

Cell Line: Hepatic stellate cells (HSCs)
Concentration: 1 nM, 10 nM, 100 nM, 1µM, 10 µM
Incubation Time: 48 hours
Result: Induced the apoptosis of HSCs.

Western Blot Analysis[2]

Cell Line: Hepatic stellate cells (HSCs)
Concentration: 1 nM, 10 nM, 100 nM, 1µM, 10 µM
Incubation Time: 48 hours
Result: Significantly increased the activation of caspase-3 and Bax in HSCs, and decreased the expression of Bcl-2. Also inhibited the activation of Akt signaling pathway.
In Vivo

Ivarmacitinib (SHR0302; 0.3-3.0 mg/kg; intragastric administration; twice a day; for 14 days; male Sprague-Dawley (SD) rats) treatment suppresses the severity of AA rats by attenuating the arthritis index, arthritis global assessment and paw swelling degree, and alleviated histopathology of spleen and joint of AA rats[1].
Ivarmacitinib can inhibit the proliferation of T, B and fibroblast-like synoviocytes (FLS), and down-regulates cytokines TNF-α, IL-1β, IL-17 and antibody IgG1, IgG2a levels, and suppresses the proportion of Th17 and total B, and inhibits JAK1-STAT3 phosphorylation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley (SD) rats (150-180 g) injected with complete Freund’s adjuvant (CFA)[1]
Dosage: 0.3 mg/kg,1.0 mg/kg, 3.0 mg/kg
Administration: Intragastric administration; twice a day; for 14 days
Result: Suppressed the severity of adjuvant-induced arthritis (AA) rats by attenuating the arthritis index, arthritis global assessment and paw swelling degree, and alleviated histopathology of spleen and joint of AA rats.
Clinical Trial
Molecular Weight

414.48

Appearance

Solid

Formula

C18H22N8O2S
CAS No.
SMILES

O=C(N1C[[email protected]@]2([H])[[email protected]@](C[[email protected]](N(C)C3=C4C(NC=C4)=NC=N3)C2)([H])C1)NC5=NC(OC)=NS5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 31.25 mg/mL (75.40 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4127 mL 12.0633 mL 24.1266 mL
5 mM 0.4825 mL 2.4127 mL 4.8253 mL
10 mM 0.2413 mL 1.2063 mL 2.4127 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.82%

COA (253 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Ivarmacitinib1445987-21-2SHR0302SHR 0302SHR-0302JAKApoptosisJanus kinaseJAK1arthritisJAK1-STAT3phosphorylationanti-proliferationTh17B-cellanti-inflammatorymigrationcollagenhepaticfibrosisInhibitorinhibitorinhibit

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