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S-Ruxolitinib (INCB018424)

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S-Ruxolitinib (INCB018424) Basic information

Product Name:
S-Ruxolitinib (INCB018424)
Synonyms:
  • S-Ruxolitinib (INCB018424)
  • S-Ruxolitinib
  • INCB 18424
  • 1H-Pyrazole-1-propanenitrile, β-cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-, (βS)-
  • Ruxolitinib (S enantioMer)
  • (3S)-3-Cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)-1H-pyrazol-1-yl]propanenitrile
  • RUXOLITINIB S ENANTIOMER;INCB18424
  • (3S)-3-Cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile (ent-Ruxolitinib)
CAS:
941685-37-6
MF:
C17H18N6
MW:
306.37
Product Categories:
  • Inhibitor
  • Inhibitors
  • Inhibitors, Pharmaceuticals, Intermediates & Fine Chemicals
  • JAK
  • STAT
Mol File:
941685-37-6.mol
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S-Ruxolitinib (INCB018424) Chemical Properties

Melting point:
138-143oC
Density 
1.40±0.1 g/cm3(Predicted)
storage temp. 
-20°C Freezer
solubility 
DMSO (Slightly), Methanol (Slightly)
form 
Solid
pka
11.63±0.50(Predicted)
color 
White
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S-Ruxolitinib (INCB018424) Usage And Synthesis

Uses

(3S)-3-Cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile is a newly developed JAK2 inhibitor therapy aimed to improve MPN-associated splenomegaly and systemic symptoms. The opposite enantiomer of Ruxolitinib (R702000).

Biological Activity

s-ruxolitinib is the chirality of incb018424, is a potent and selective small-molecule janus kinase 1 (jak1) and jak2 inhibitor. it was initially developed to target the constitutive activation of the jak-stat pathway. janus kinases (jaks) are a family of cytoplasmic tyrosine kinases that mediates signals from the receptors for various cytokines and growth factors that have a key role in haematopoiesis and immune function. ruxolitinib maintains its anti-jak activity by competitive inhibition of the atp-binding catalytic site of the kinase domain. ruxolitinib is well absorbed at >95%. exposure of jak2v617f-positive ba/f3 cells to ruxolitinib iss shown to result in reduced cellular proliferation.ruben a. mesa, uma yasothan, peter kirkpatrick. ruxolitinib. nature reviews drug discovery. 2012; 11: 103-104john mascarenhas, ronald hoffman. ruxolitinib: the first fda approved therapy for the treatment of myelofibrosis. clinical cancer research. 2012; 18(11): 3008 - 3014

in vivo

Ruxolitinib (S enantiomer) (S-Ruxolitinib; 30 mg/kg; Oral gavage; twice per day separated 10-12 h for 8 weeks) reduces haematopoietic cell expansion in MPN[2].

Animal Model:Female wild-type C57BL/6J or Nes-gfp27 mice with myeloproliferative neoplasms (MPNs) in peripheral blood[2]
Dosage:30 mg/kg (in 0.5% hydroxypropylmethylcellulose after solubilisation in DMSO)
Administration:Oral gavage; twice per day separated 10-12 h for 8 weeks
Result:Reduced haematopoietic cell expansion in MPN but it did not rescue bone marrow (BM) mesenchymal stem cells (MSCs).

target

JAK1

IC 50

JAK

S-Ruxolitinib (INCB018424)Supplier

J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Email
jkinfo@jkchemical.com
Jinan Trio PharmaTech Co., Ltd.
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0531-88811783
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sales@trio-pharmatech.com
Daicel Chiral Technologies (China)CO.,LTD
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021-50460086-9 15921403865
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han_yajun@dctc.daicel.com
BOC Sciences
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1-631-485-4226; 16314854226
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info@bocsci.com
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
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