AZD-1208 - CAS 1204144-28-4
Catalog number: 1204144-28-4
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
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AZD1208 is orally available, small molecule inhibitor of PIM kinases with potential antineoplastic activity. AZD1208 inhibits the activities of PIM1, PIM2 and PIM3 serine/threonine kinases, which may result in the interruption of the G1/S phase cell cycle transition.
Light yellow solid powder
AZD1208; AZD 1208.
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1.Targeting of glioblastoma cell lines and glioma stem cells by combined PIM kinase and PI3K-p110α inhibition.
Iqbal A1,2, Eckerdt F1, Bell J1,3, Nakano I4, Giles FJ1,3, Cheng SY1, Lulla RR1,2, Goldman S1,2, Platanias LC1,3,5. Oncotarget. 2016 Apr 21. doi: 10.18632/oncotarget.8899. [Epub ahead of print]
The PIM family of proteins encodes serine/threonine kinases with important roles in protein synthesis and cancer cell metabolism. In glioblastoma (GBM) cell lines, siRNA-mediated knockdown of PIM kinases or pharmacological inhibition of PIM kinases by SGI-1776 or AZD-1208 results in reduced phosphorylation of classic PIM effectors and also elements of the PI3K/mTOR pathway, suggesting interplay between PIM and mTOR signals in GBM cells. Combination of PIM kinase inhibitors with BYL-719, an inhibitor specific for the PI3K catalytic isoform p110α, results in enhanced antineoplastic effects in GBM cells. Additionally, pharmacologic inhibition of PIM kinases impairs growth of patient-derived glioma sphere cells, suggesting an important role for PIM kinases in cancer stem cell (CSC) function and survival. Such effects are further enhanced by concomitant inhibition of PIM kinase and p110α activities. Altogether these findings suggest that pharmacological PIM targeting in combination with PI3K inhibition may provide a unique therapeutic approach for the treatment of heterogeneous tumors containing populations of therapy-resistant CSCs in GBM.
2.Combination of Pim kinase inhibitors and Bcl-2 antagonists in chronic lymphocytic leukemia cells.
Cervantes-Gomez F1, Lavergne B1, Keating MJ2, Wierda WG2, Gandhi V1,2. Leuk Lymphoma. 2015 Sep 28:1-9. [Epub ahead of print]
The Pim proteins are Ser/Thr kinases over-expressed in several hematological malignancies such as chronic lymphocytic leukemia (CLL) and some solid cancers like prostate cancer. Several small molecules have been developed to inhibit these kinases. In prostate cancer cell lines, the Pim kinase inhibitor SMI-4a and the Bcl-2 antagonist ABT-737 resulted in synergistic cytotoxicity. Akin to prostate cancer cells, CLL lymphocytes over-express Pim and Bcl-2 proteins. It was hypothesized that similar cytotoxic interaction should be observed in CLL. This study evaluated the in vitro cytotoxic effect of three Pim kinase inhibitors (AZD1208, SGI-1776 and SMI-4a) combined with Bcl-2 antagonists (ABT-737 or ABT-199) in malignant CLL lymphocytes. Data indicated Pim kinase inhibitors in combination with ABT-737 or ABT-199 resulted mostly in additive cytotoxicity with a few synergistic responses; however, the extent of synergism was less robust than that observed previously in prostate cancer cell lines treated with SMI-4a and ABT-737.
3.The PIM inhibitor AZD1208 synergizes with ruxolitinib to induce apoptosis of ruxolitinib sensitive and resistant JAK2-V617F-driven cells and inhibit colony formation of primary MPN cells.
Mazzacurati L1, Lambert QT1, Pradhan A1, Griner LN1, Huszar D1,2, Reuther GW1. Oncotarget. 2015 Nov 24;6(37):40141-57. doi: 10.18632/oncotarget.5653.
Classical myeloproliferative neoplasms (MPNs) are hematopoietic stem cell disorders that exhibit excess mature myeloid cells, bone marrow fibrosis, and risk of leukemic transformation. Aberrant JAK2 signaling plays an etiological role in MPN formation. Because neoplastic cells in patients are largely insensitive to current anti-JAK2 therapies, effective therapies remain needed. Members of the PIM family of serine/threonine kinases are induced by JAK/STAT signaling, regulate hematopoietic stem cell growth, protect hematopoietic cells from apoptosis, and exhibit hematopoietic cell transforming properties. We hypothesized that PIM kinases may offer a therapeutic target for MPNs. We treated JAK2-V617F-dependent MPN model cells as well as primary MPN patient cells with the PIM kinase inhibitors SGI-1776 and AZD1208 and the JAK2 inhibitor ruxolitinib. While MPN model cells were rather insensitive to PIM inhibitors, combination of PIM inhibitors with ruxolitinib led to a synergistic effect on MPN cell growth due to enhanced apoptosis.
4.Loss of PIM2 enhances the anti-proliferative effect of the pan-PIM kinase inhibitor AZD1208 in non-Hodgkin lymphomas.
Kreuz S1, Holmes KB2, Tooze RM3, Lefevre PF4. Mol Cancer. 2015 Dec 8;14:205. doi: 10.1186/s12943-015-0477-z.
BACKGROUND: A promising therapeutic approach for aggressive B-cell Non-Hodgkin lymphoma (NHL), including diffuse large B-cell lymphoma (DLBCL), and Burkitt lymphoma (BL) is to target kinases involved in signal transduction and gene regulation. PIM1/2 serine/threonine kinases are highly expressed in activated B-cell-like DLBCL (ABC-DLBCL) with poor prognosis. In addition, both PIM kinases have a reported synergistic effect with c-MYC in mediating tumour development in several cancers, c-MYC gene being translocated to one of the immunoglobulin loci in nearly all BLs.
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CAS 1204144-28-4 AZD-1208

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