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Ruxolitinib

Item № 11609
CAS № 941678-49-5
Purity ≥98%
product image
                (CAS 941678-49-5)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $25.00 0.00
     5 mg $113.00 0.00
     10 mg $213.00 0.00
     25 mg $344.00 0.00

Pricing updated 2019-07-18. Prices are subject to change without notice.

Description
Synonyms
  • INCB 018424

Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors.1,2 A JAK2 gene fusion mutation, JAK2V617F, that causes unchecked activation of various growth factors and cytokines, has been linked to myeloproliferative neoplasms (MPNs), including polycythemia vera, essential thrombocythemia, and primary myelofibrosis.3 Ruxolitinib is a potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5 nM, respectively and is relatively less selective for JAK3 (IC50 = 322 nM).3 It can block interleukin-6 (IL-6) signaling (IC50 = 281 nM) and proliferation of JAK2V617F+ Ba/F3 cells (IC50 = 127 nM).4 In primary cultures, ruxolitinib preferentially suppresses erythroid progenitor colony formation from JAK2V617F+ polycythemia vera patients (IC50 = 67 nM) versus healthy donors (IC50 > 400 nM).4 In a mouse model of JAK2V617F+ MPN, 90 mg/kg ruxolitinib reduced splenomegaly, decreased circulating levels of IL-6 and TNF-α, eliminated neoplastic cells, and prolonged survival of the treated animals.4

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Technical Information
Formal Name
βR-cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile
CAS Number
941678-49-5
Synonyms
  • INCB 018424
Molecular Formula
C17H18N6
Formula Weight
306.4
Purity
≥98%
Formulation
A crystalline solid
λmax
216, 224, 253, 309 nm
SMILES
N#CC[C@H](C1CCCC1)N(N=C2)C=C2C3=C4C(NC=C4)=NC=N3
InChI Code
InChI=1S/C17H18N6/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16/h6,8-12,15H,1-5H2,(H,19,20,21)/t15-/m1/s1
InChI Key
HFNKQEVNSGCOJV-OAHLLOKOSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
Downloads & Resources
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Additional Information

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References & Product Citations
Product Description References

1. Leonard, W.J., and O'Shea, J.J. JAKS AND STATS: Biological implications Annual Reviews of Immunology 16, 293-322 (1998).

2. Yamaoka, K., Saharinen, P., Pesu, M., et al. The janus kinases (Jaks) Genome Biology 5(12), 1-6 (2004).

3. Verstovsek, S. Therapeutic potential of JAK2 inhibitors Hematology Am.Soc.Hematol.Educ.Program 2009(1), 636-642 (2009).

4. Quintás-Cardama, A., Vaddi, K., Liu, P., et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: Therapeutic implications for the treatment of myeloproliferative neoplasms Blood 115(15), 3109-3117 (2010).

Product Citations

Wang, W., Green, M., Choi, J.E., et al. CD8+ T cells regulate tumour ferroptosis during cancer immunotherapy Nature 569(7755), 270-274 (2019).

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