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Ruxolitinib phosphate

Catalog No. T3043   CAS 1092939-17-7
Synonyms: INC424, INCB018424, INC 424 phosphate, Ruxolitinib (INCB-18424) phosphate, INCB018424 phosphate

Ruxolitinib phosphate (INCB018424)(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, <130-fold selectivity for JAK1/2 versus JAK3.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Ruxolitinib phosphate Chemical Structure
Ruxolitinib phosphate, CAS 1092939-17-7
Pack Size Availability Price/USD Quantity
5 mg In stock $ 44.00
10 mg In stock $ 59.00
25 mg In stock $ 75.00
50 mg In stock $ 98.00
100 mg In stock $ 148.00
200 mg In stock $ 239.00
500 mg In stock $ 439.00
1 g In stock $ 648.00
1 mL * 10 mM (in DMSO) In stock $ 54.00
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Purity: 100%
Purity: 99.86%
Purity: 99.86%
Purity: 99.72%
Purity: 99.67%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ruxolitinib phosphate (INCB018424)(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.
Targets&IC50 JAK2:2.8 nM, JAK1:3.3 nM
In vitro Ruxolitinib (INCB018424) potently and selectively inhibits JAK2V617F-mediated signaling and proliferation. Ruxolitinib inhibits the growth of HEL cells with EC50 of 186 nM. Ruxolitinib markedly increases apoptosis in Ba/F3-EpoR-JAK2V617F cell system. It also inhibits hematopoietic progenitor cell proliferation in primary MPN patient samples[1].
In vivo Ruxolitinib (180 mg/kg, p.o.) reduces the tumor burden of mice inoculated with JAK2V617F-expressing cells while not causing anemia or lymphopenia[1].
Cell Research Ruxolitinib phosphate is dissolved in 0.2% DMSO. Cells are seeded at 2000/well of white bottom 96-well plates, treated with compounds from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37°C with 5% CO2. Viability is measured by cellular ATP determination using the Cell-Titer Glo luciferase reagent or viable cell counting. Values are transformed to percent inhibition relative to vehicle control, and IC50?curves are fitted according to nonlinear regression analysis of the data using PRISM GraphPad.
Synonyms INC424, INCB018424, INC 424 phosphate, Ruxolitinib (INCB-18424) phosphate, INCB018424 phosphate
Molecular Weight 404.36
Formula C17H21N6O4P
CAS No. 1092939-17-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 70 mg/mL(173.1 mM)

H2O: 8 mg/mL(19.8 mM)

TargetMolReferences and Literature

1. Quintas-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood, 2010, 115(15), 3109-3117. 2. Gao C, Yan Y, Chen G, et al. Autophagy Activation Represses Pyroptosis through the IL-13 and JAK1/STAT1 Pathways in a Mouse Model of Moderate Traumatic Brain Injury[J]. ACS Chemical Neuroscience. 2020 3. Zhang M, Yang W, Wang P, et al. CCL7 recruits cDC1 to promote antitumor immunity and facilitate checkpoint immunotherapy to non-small cell lung cancer[J]. Nature communications. 2020, 11(1): 1-17.

TargetMolCitations

1. Zhang M, Yang W, Wang P, et al. CCL7 recruits cDC1 to promote antitumor immunity and facilitate checkpoint immunotherapy to non-small cell lung cancer. Nature communications. 2020, 11(1): 1-17 2. Gao C, Yan Y, Chen G, et al. Autophagy Activation Represses Pyroptosis through the IL-13 and JAK1/STAT1 Pathways in a Mouse Model of Moderate Traumatic Brain Injury. ACS Chemical Neuroscience. 2020

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Tyrosine Kinase Inhibitor Library Approved Drug Library Bioactive Compounds Library Max Angiogenesis related Compound Library Bioactive Compound Library Anti-Pancreatic Cancer Compound Library Pediatric Drug Library

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Keywords

Ruxolitinib phosphate 1092939-17-7 Angiogenesis Autophagy Chromatin/Epigenetic JAK/STAT signaling Stem Cells Mitophagy JAK Ruxolitinib inhibit INCB 018424 Phosphate INCB 018424 INCB-018424 INC424 INC424 Phosphate Mitochondrial Autophagy Ruxolitinib Phosphate INCB018424 INC 424 phosphate INC 424 INC-424 Phosphate Inhibitor INC 424 Phosphate INCB-018424 Phosphate INCB018424 Phosphate Ruxolitinib (INCB-18424) phosphate INCB018424 phosphate Ruxolitinib (INCB-18424) Phosphate INC-424 Janus kinase inhibitor

 

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