INCB16562
WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#:406192
CAS#:933768-63-9
Description:INCB16562 is a novel, selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3. Treatment of myeloma cells with INCB16562 potently inhibited interleukin-6 (IL-6)-induced phosphorylation of STAT3. INCB16562 abrogated the protective effects of recombinant cytokines or bone marrow stromal cells and sensitized myeloma cells to cell death by exposure to dexamethasone, melphalan, or bortezomib. Oral administration of INCB16562 antagonized the growth of myeloma xenografts in mice and enhanced the antitumor activity of relevant agents in combination studies. INCB16562 is a potent JAK1/2 inhibitor and that mitigation of JAK/STAT signaling by targeting JAK1 and JAK2 will be beneficial in the treatment of myeloma patients, particularly in combination with other agents. ( source: Neoplasia. 2010 Jan;12(1):28-38. ).
Price and Availability
INCB16562 is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.
Chemical Structure
Theoretical Analysis
MedKoo Cat#: 406192Name: INCB16562CAS#: 933768-63-9Chemical Formula: C19H11Cl2N5Exact Mass: 379.03915Molecular Weight: 380.23Elemental Analysis: C, 60.02; H, 2.92; Cl, 18.65; N, 18.42
Synonym:INCB16562; INCB-16562; INCB 16562.
IUPAC/Chemical Name:2-(2,6-dichlorophenyl)-1,8-dihydroimidazo[4,5-d]dipyrido[2,3-b:4',3'-f]azepine
InChi Key:DVCPYUTZIIXGFE-UHFFFAOYSA-N
InChi Code:InChI=1S/C19H11Cl2N5/c20-12-4-1-5-13(21)15(12)19-25-16-10-6-8-22-9-14(10)24-18-11(17(16)26-19)3-2-7-23-18/h1-9H,(H,23,24)(H,25,26)
SMILES Code:ClC1=C(C(N2)=NC3=C2C4=CC=CN=C4NC5=CN=CC=C35)C(Cl)=CC=C1
Technical Data
Additional Information
References
1: Koppikar P, Abdel-Wahab O, Hedvat C, MarubayashiS, Patel J, Goel A, Kucine N, Gardner JR, Combs AP, Vaddi K, Haley PJ, Burn TC, Rupar M, Bromberg JF,Heaney ML, de Stanchina E, Fridman JS, Levine RL. Efficacy of the JAK2inhibitor INCB16562 in a murine model of MPLW515L-induced thrombocytosis andmyelofibrosis. Blood. 2010 Apr 8;115(14):2919-27. doi: 10.1182/blood-2009-04-218842.Epub 2010 Feb 12. PubMed PMID: 20154217; PubMed Central PMCID: PMC2854434.
2: Li J, Favata M, Kelley JA, Caulder E, Thomas B, Wen X, Sparks RB,Arvanitis A, Rogers JD, Combs AP, Vaddi K, Solomon KA, Scherle PA, Newton R, FridmanJS. INCB16562, a JAK1/2 selective inhibitor, is efficacious against multiplemyelomacells and reverses the protective effects of cytokine and stromal cellsupport. Neoplasia. 2010 Jan;12(1):28-38. PubMed PMID: 20072651; PubMed CentralPMCID: PMC2805881.
3: Liu PC, Caulder E, Li J, Waeltz P, Margulis A, Wynn R, Becker-PashaM, Li Y, Crowgey E, Hollis G, Haley P, Sparks RB, Combs AP, Rodgers JD, Burn TC,Vaddi K,Fridman JS. Combined inhibition of Janus kinase 1/2 for the treatment of JAK2V617F-driven neoplasms: selective effects on mutant cells andimprovements in measures of disease severity. Clin Cancer Res. 2009 Nov15;15(22):6891-900. doi:10.1158/1078-0432.CCR-09-1298. Epub 2009 Nov 3. PubMed PMID: 19887489.
