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Ruxolitinib, Purified Small Molecule
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Catalog Number
PE-1856
Discontinued
- Product Name Ruxolitinib, Purified Small Molecule
- Product Description Ruxolitinib dihydrochloride is a specific inhibitor of Janus-associated kinase (JAK1 and JAK2). Ruxolitinib is a small molecular with the formula of C17H21N6O4Pand Molecular Weight of 404. Ruxolitinib phosphate is an administered ATP-competitive cyclopentylpropionitrile derivative and shows inhibition activity on JAK1 and JAK2. Ruxolitinib inhibits phosphorylation of JAK1/2, STAT5, and ERK1/2, resulting in reduced cellular proliferation
- Alternative Names INCB018424; CAS #:941678-49-5; INCB-018424
- Application(s) Neutralize
- Purity Description >98% (HPLC); NMR (Conforms)
- Purity % > 98%
- Regulatory Status For research use only.
Product Info
- Product Description Ruxolitinib dihydrochloride is a specific inhibitor of Janus-associated kinase (JAK1 and JAK2). Ruxolitinib is a small molecular with the formula of C17H21N6O4Pand Molecular Weight of 404. Ruxolitinib phosphate is an administered ATP-competitive cyclopentylpropionitrile derivative and shows inhibition activity on JAK1 and JAK2. Ruxolitinib inhibits phosphorylation of JAK1/2, STAT5, and ERK1/2, resulting in reduced cellular proliferation
- Application(s) Neutralize
- Application Details Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
- Target Ruxolitinib
- Target Host Species Species Independent
- Purity Description >98% (HPLC); NMR (Conforms)
- Purity % > 98%
- Format Dry powder; Off-white powder
- Reconstitution Instructions Soluble in DMSO. May be dissolved in DMSO up to 28 mg/mL or 15 mg/mL ethanol
- Storage Instructions Store desiccated as supplied at -20°C for up to 2 years. Store solutions at -20°C for up to 1 month. Prevent multiple freeze-thaw cycles.
- Batch Number Please see item label.
- Expiration Date See storage conditions.
- Alternative Names INCB018424; CAS #:941678-49-5; INCB-018424
- Scientific Background Pharmacology: Potent and selective JAK1&2 inhibitor, IC50s=2.7, 4.5 and 322 nM for JAK1, JAK2 and JAK3 respectively (1). Blocks IL-6 signaling (IC50=281 nM) and proliferation of JAK2V617F+ Ba/F3 cells (IC50=127 nM) (2). Inhibits the proinflammatory secretome of senescent cells (3). The JAK1 S646P mutant is sensitive to ruxolitinib (4). Clinically useful anticancer agent. PubChem CID: 2512798 Product is sold for research use only. Not for human therapeutic use or for medicinal purposes
- Shipping Temperature 25°C (ambient)
- UNSPSC CODE 12352401
- Regulatory Status For research use only.
Specifications
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General References
S Verstovsek et al. Hematol. Am. Soc. Hematol. Educ. Program 2009 2009(1)636
A Quintas-Cardama et al. Blood 2010 115:3109
JN Farr et al. Nat. Med. 2017 23:1072
Q Li et al. Oncotarget 2017 8:34687