| Identification | Back Directory | [Name]
S-Ruxolitinib (INCB018424) | [CAS]
941685-37-6 | [Synonyms]
CS-1401 INCB 18424 S-Ruxolitinib Ruxolitinib Impurity A S-Ruxolitinib (INCB018424) Ruxolitinib (S enantioMer) RUXOLITINIB S ENANTIOMER;INCB18424 Ruxolitinib Impurity 1((S)-Ruxolitinib) (S)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile 1H-Pyrazole-1-propanenitrile, β-cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-, (βS)- (3S)-3-Cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)-1H-pyrazol-1-yl]propanenitrile (3S)-3-Cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile (ent-Ruxolitinib) | [Molecular Formula]
C17H17N6 | [MDL Number]
MFCD13184797 | [MOL File]
941685-37-6.mol | [Molecular Weight]
305.357 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. | [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 myelo?brosis. 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 |
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| Company Name: |
J & K SCIENTIFIC LTD.
|
| Telephone: |
18210857532 18210857532 |
| Website: |
https://www.jkchemical.com |
| Company Name: |
NCE Biomedical Co.,Ltd.
|
| Telephone: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
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