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Ivarmacitinib

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].

Product Specifications

CAS Number

[1445987-21-2]

Product Name Alternative

SHR0302

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; JAK

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/ivarmacitinib.html

Concentration

10mM

Purity

99.62

Solubility

DMSO : 31.25 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C18H22N8O2S

Molecular Weight

414.48

Precautions

H302, H315, H319, H335

References & Citations

[1]Huaxun Wu, et al. JAK1-STAT3 Blockade by JAK Inhibitor SHR0302 Attenuates Inflammatory Responses of Adjuvant-Induced Arthritis Rats and Decreases Th17 and Total B Cells. Joint Bone Spine. 2016 Oct;83 (5) :525-32.|[2]Yuan-Jing Gu, et al. Targeted Blockade of JAK/STAT3 Signaling Inhibits Proliferation, Migration and Collagen Production as Well as Inducing the Apoptosis of Hepatic Stellate Cells. Int J Mol Med. 2016 Sep;38 (3) :903-11.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

JAK1; JAK2; JAK3; Tyk2

Available Sizes

Curated Selection

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