AZD1208
AZD1208
AZD1208
| Catalog | Description | Size | Price (USD) | Qty |
|---|---|---|---|---|
| GBM-4781-5MG | AZD1208 | 5mg | $116.00 | |
| GBM-4781-25MG | AZD1208 | 25mg | $410.00 |
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Description
pan-PIM kinase inhibitor
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Specifications
Bioassays Specification Bio-Activity pan-PIM kinase inhibitor Chemical Name (5Z)-5-[[2-[(3R)-3-Aminopiperidin-1-yl]-3-phenylphenyl]methylidene]-1,3-thiazolidine-2,4-dione Function / Pharmacology Highly selective and potent pan-PIM kinase inhibitor (IC50 = 3 nM PIM1; 150 nM PIM2; 9 nM PIM3).1 Displayed efficacy in models of acute myeloid leukemia2, prostate cancer3, and triple-negative breast cancer4. Combination treatment of AZD1208 and imatinib eliminated chronic myelogenous leukemia stem cells in cell culture and a patient-derived mouse xenograft model.5 It improved immunotherapeutic antitumor T-cell response6 and disrupted the myeloid cell-mediated immunosuppressive tumor microenvironment increasing T-cell-mediated antitumor immunity. CAS# 1204144-28-4 MW 379.48 Molecular Formula C21H21N3O2S Purity >98% Solubility Soluble in DMSO (up to 2 mg/ml) with warming Supplied powder Storage as supplied -20°C Ship temp Ambient References 1) Dakin et al. (2012), Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases; Bioorg. Med. Chem. Lett. 22 4599 2) Keeton et al. (2014), AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia; Blood 123 905 3) Kirschner et al. (2014), PIK kinase inhibitor AZD1208 for treatment of MYC-driven prostate cancer; J. Natl. Cancer Inst. 107 dju407 4) Braso-Maristany et al. (2016), PIM1 kinase regulates cell death, tumor growth and chemotherapy response in triple-negative breast cancer; Nat. Med. 22 1303 5) Ma et al. (2019), Prosurvival kinase PIM2 is a therapeutic target for eradication of chronic myeloid leukemia stem cells; Proc.Natl. Acad. Sci. USA 116 10482 6) Chatterjee et al. (2019), Targeting PIM Kinase with PD1 Inhibition Improves Immunotherapeutic Antitumor T-cell Response; Clin. Cancer Res. 25 1036 7) Xin et al. (2021), Targeting PIM1-Mediated Metabolism in Myeloid Suppressor Cells to Treat Cancer; Cancer Immunol. Res. 9 454 - Reviews
| Bioassays Specification | |
| Bio-Activity | pan-PIM kinase inhibitor |
| Chemical Name | (5Z)-5-[[2-[(3R)-3-Aminopiperidin-1-yl]-3-phenylphenyl]methylidene]-1,3-thiazolidine-2,4-dione |
| Function / Pharmacology | Highly selective and potent pan-PIM kinase inhibitor (IC50 = 3 nM PIM1; 150 nM PIM2; 9 nM PIM3).1 Displayed efficacy in models of acute myeloid leukemia2, prostate cancer3, and triple-negative breast cancer4. Combination treatment of AZD1208 and imatinib eliminated chronic myelogenous leukemia stem cells in cell culture and a patient-derived mouse xenograft model.5 It improved immunotherapeutic antitumor T-cell response6 and disrupted the myeloid cell-mediated immunosuppressive tumor microenvironment increasing T-cell-mediated antitumor immunity. |
| CAS# | 1204144-28-4 |
| MW | 379.48 |
| Molecular Formula | C21H21N3O2S |
| Purity | >98% |
| Solubility | Soluble in DMSO (up to 2 mg/ml) with warming |
| Supplied | powder |
| Storage as supplied | -20°C |
| Ship temp | Ambient |
| References | 1) Dakin et al. (2012), Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases; Bioorg. Med. Chem. Lett. 22 4599 2) Keeton et al. (2014), AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia; Blood 123 905 3) Kirschner et al. (2014), PIK kinase inhibitor AZD1208 for treatment of MYC-driven prostate cancer; J. Natl. Cancer Inst. 107 dju407 4) Braso-Maristany et al. (2016), PIM1 kinase regulates cell death, tumor growth and chemotherapy response in triple-negative breast cancer; Nat. Med. 22 1303 5) Ma et al. (2019), Prosurvival kinase PIM2 is a therapeutic target for eradication of chronic myeloid leukemia stem cells; Proc.Natl. Acad. Sci. USA 116 10482 6) Chatterjee et al. (2019), Targeting PIM Kinase with PD1 Inhibition Improves Immunotherapeutic Antitumor T-cell Response; Clin. Cancer Res. 25 1036 7) Xin et al. (2021), Targeting PIM1-Mediated Metabolism in Myeloid Suppressor Cells to Treat Cancer; Cancer Immunol. Res. 9 454 |