Day: March 10, 2014

RUXOLITINIB…FOR THE TREATMENT OF INT OR HIGH-RISK MYELOFIBROSIS

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New Drug Approvals

Ruxolitinib

(3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile, cas no 941678-49-5

(R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile

  • 1H-Pyrazole-1-propanenitrile, beta-cyclopentyl-4-(7H-pyrrolo(2,3-d)pyrimidin-4-yl)-,(betaR)-

Formula: C17H18N6Molecular Weight: 306.37

JAKAFI® (ruxolitinib) Structural Formula Illustration

Phosphate salt

(R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate

INCB 018424

  • INCB 018424
  • INCB018424
  • Ruxolitinib
  • UNII-82S8X8XX8H

CAS No.: 1092939-17-7
M.Wt: 404.36
Formula: C17H21N6O4P
Ruxolitinib phosphate

LAUNCHED 2011, INCYTE FOR MYELOFIBROSIS, NDA202192, 2011-11-16

CLINICAL TRIALS.http://clinicaltrials.gov/search/intervention=INCB018424+OR+ruxolitinib

EMA:Link,

US FDA:link

HPLC, MS, NMR…http://www.medkoo.com/Product-Data/Ruxolitinib/Ruxolitinib-QC-LC20130225.pdf

http://file.selleckchem.com/downloads/nmr/S137803-INCB018424-HNMR-Selleck.pdf

http://file.selleckchem.com/downloads/hplc/S137803-INCB018424-HPLC-Selleck.pdf

Ruxolitinib phosphate is a kinase inhibitor with the chemical name (R)-3-(4-(7H-pyrrolo[2,3d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate and a molecular weight of 404.36.

Ruxolitinib is a janus-associated kinase inhibitor indicated to treat bone marrow cancer, specifically intermediate or high-risk myelofibrosis. FDA approved on November 16, 2011.

INCB018424 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

Ruxolitinib phosphate has the following structural formula:

JAKAFI® (ruxolitinib) Structural Formula Illustration

Ruxolitinib phosphate is a white to off-white to light pink powder…

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