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. ).

MedKoo Cat#: 406192 Name: INCB16562 CAS#: 933768-63-9 Chemical Formula: C19H11Cl2N5 Exact Mass: 379.03915 Molecular Weight: 380.23 Elemental 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

Appearance: Solid powder

Purity: >98%

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

Additional Information

        

References

1: Koppikar P, Abdel-Wahab O, Hedvat C, Marubayashi S, 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 JAK2 inhibitor INCB16562 in a murine model of MPLW515L-induced thrombocytosis and myelofibrosis. 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, Fridman JS. INCB16562, a JAK1/2 selective inhibitor, is efficacious against multiple myeloma cells and reverses the protective effects of cytokine and stromal cell support. Neoplasia. 2010 Jan;12(1):28-38. PubMed PMID: 20072651; PubMed Central PMCID: PMC2805881.

3: Liu PC, Caulder E, Li J, Waeltz P, Margulis A, Wynn R, Becker-Pasha M, 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 and improvements in measures of disease severity. Clin Cancer Res. 2009 Nov 15;15(22):6891-900. doi: 10.1158/1078-0432.CCR-09-1298. Epub 2009 Nov 3. PubMed PMID: 19887489.

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