AZD1208
Based on 22 publication(s) in Google Scholar
AZD1208 is an orally bioavailable, highly selective PIM kinases inhibitor.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.73%
- No. CAS: 1204144-28-4
- Fòrmula: C21H21N3O2S
- Peso molecular:379.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) AZD1208
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Nat Commun. 2019 Apr 23;10(1):1844. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Adv Sci (Weinh). 2025 Jul 6:e03487. [Abstract]
- Cell Chem Biol. 2024 Feb 15;31(2):326-337.e11. [Abstract]
- Neurosci Bull. 2024 Dec;40(12):1901-1914. [Abstract]
- Biochem Pharmacol. 2026 Jan;243(Pt 2):117536. [Abstract]
- mBio. 2025 Oct 8;16(10):e0168025. [Abstract]
- Int Immunopharmacol. 2023 Jan:114:109563. [Abstract]
- Cell Signal. 2024 Jan:113:110969. [Abstract]
- PLoS Negl Trop Dis. 2026 Jan 20;20(1):e0013915. [Abstract]
- eNeuro. 2019 Aug 22;6(4):ENEURO.0003-19.2019. [Abstract]
- PLoS One. 2025 Nov 12;20(11):e0335501. [Abstract]
- Prostate. 2025 Apr 23. [Abstract]
- Exp Ther Med. 2022 Jan;23(1):81. [Abstract]
- bioRxiv. 2025 Nov 3:2025.10.31.685966. [Abstract]
- bioRxiv. 2024 Nov 6:2024.11.04.621884. [Abstract]
- bioRxiv. 2024 Mar 28.
- Research Square Preprint. 2024 Feb 16.
- The University of Chicago. 2021 Apr.
- Charles University. 2019 Jun.
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
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Actividad biológica
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PIM2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KMS-11 | EC50 |
0.67 μM
Compound: 2; AZD1208
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Antiproliferative activity against luciferase expressing human KMS11 cells after 72 hrs by Cell-TiterGlo assay
Antiproliferative activity against luciferase expressing human KMS11 cells after 72 hrs by Cell-TiterGlo assay
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[PMID: 26505898] |
| WI-38 | IC50 |
>10000 nM
Compound: AZD1208
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Growth inhibition of human WI38 cells after 48 hrs by CCK8 assay
Growth inhibition of human WI38 cells after 48 hrs by CCK8 assay
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[PMID: 28523101] |
AZD1208 shows good antiproliferative activity in a megakaryoblastic leukemia cell line, MOLM-16, with GI50 values less than 100 nM[1].
AZD1208 (10 μM) inhibits the growth of Ramos cells, and at 1 μM, strongly inhibits PIM kinases in all cell at 1 μM. AZD1208 induces apoptosis, and PIM2 knockdown is mainly associated with an alteration of the cell cycle[2].
The combination of AZD1208 and AZD2014 rapidly activates AMPKα, a negative regulator of translation machinery through mTORC1/2 signaling in AML cells; profoundly inhibits AKT and 4EBP1 activation; and suppresses polysome formation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1204144-28-4
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Appearance Solid
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Peso molecular 379.48
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Fòrmula C21H21N3O2S
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Color Light yellow to yellow
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SMILES
O=C(NC/1=O)SC1=C/C2=C(N3C[C@H](N)CCC3)C(C4=CC=CC=C4)=CC=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (22)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Nat Commun
PIM kinases facilitate lentiviral evasion from SAMHD1 restriction via Vpx phosphorylation. [Abstract]2019 Apr 23;10(1):1844. PMID: 31015445
AZD1208 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Apr 23;10(1):1844. [Abstract]
Primary monocytes were differentiated into macrophages and infected with HIV-2 reporter virus carrying wild-type Vpx or its S13A mutants. A pan-PIM kinase inhibitor AZD1208 (0, 0.1, 0.5 μM) was added 4 h before infection. Fortyeight hours post-infection, cells were harvested and subjected to luciferase assay.
AZD1208 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Apr 23;10(1):1844. [Abstract]
Primary monocytes were differentiated into macrophages and infected with HIV-2 reporter virus carrying wild-type Vpx or its S13A mutants. A pan-PIM kinase inhibitor AZD1208 (0, 0.1, 0.5 μM) was added 4 h before infection. Fortyeight hours post-infection, cells were harvested and immunoblotting to measure HIV-2 infectivity and SAMHD1 expression.
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Adv Sci (Weinh)
PIM1 Attenuates Innate Immunity to Foster Coronavirus Replication through Ubiquitin Ligase β-TrCP-Mediated IFNAR1 Degradation. [Abstract]2025 Jul 6:e03487. PMID: 40619619
AZD1208 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 6:e03487. [Abstract]
Protein level of p-STAT1/2 in HEK293T cells treated with PIM1 inhibitor AZD-1208 (0, 2, 4, 8 μM) for 24h followed by the stimulation with/without poly: IC for 16 h, or IFN for 1h.
AZD1208 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 6:e03487. [Abstract]
PIM inhibitors AZD-1208 (0-12 μM) pre-treated with RD cells for 2h, followed by the OC43 infection for 72h at the MOI of 0.01. OC43 viral RNA were determined.
AZD1208 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 6:e03487. [Abstract]
PIM inhibitors AZD-1208 (0-12 μM) pre-treated with RD cells for 2h, followed by the OC43 infection for 72h at the MOI of 0.01. OC43 viral N protein was determined.
AZD1208 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 6:e03487. [Abstract]
Protein level of -TrCP1 in HEK293T cells treated with the indicated concentration of PIM1 inhibitor AZD-1208 (0-12 μM) for 48h.
AZD1208 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 6:e03487. [Abstract]
Western blot for IFNAR1 expression in HEK293T or HepG2 cells treated with PIM1 inhibitors AZD-1208 (0, 2, 4, 8 μM) for 48 h.
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Cell Chem Biol
2024 Feb 15;31(2):326-337.e11. PMID: 38016478 -
Neurosci Bull
Melatonin Ameliorates Abnormal Sleep-Wake Behavior via Facilitating Lipid Metabolism in a Zebrafish Model of Parkinson's Disease. [Abstract]2024 Dec;40(12):1901-1914. PMID: 39283564 -
Biochem Pharmacol
Targeting PIM1 ameliorates sepsis-associated acute kidney injury through inhibiting ferroptosis. [Abstract]2026 Jan;243(Pt 2):117536. PMID: 41207569 -
mBio
PIM1 orchestrates sepsis-associated inflammatory imbalance in CD4+ T cell subsets via cholesterol metabolism. [Abstract]2025 Oct 8;16(10):e0168025. PMID: 40899834 -
Int Immunopharmacol
2023 Jan:114:109563. PMID: 36513021 -
Cell Signal
2024 Jan:113:110969. PMID: 37967691 -
PLoS Negl Trop Dis
Unraveling the role of host kinase PIM1 in Toxoplasma gondii infection: Implications for therapies. [Abstract]2026 Jan 20;20(1):e0013915. PMID: 41557744 -
eNeuro
2019 Aug 22;6(4):ENEURO.0003-19.2019. PMID: 31387876 -
PLoS One
PIM1 induces hypoxia-related fibroblast senescence in a mouse model of stress urinary incontinence. [Abstract]2025 Nov 12;20(11):e0335501. PMID: 41223182 -
Prostate
Valosin-Containing Protein (VCP/p97) Mediates Neuroendocrine Differentiation in Prostate Cancer Cells Through Pim1 Signaling Inducing Autophagy. [Abstract]2025 Apr 23. PMID: 40269472 -
Exp Ther Med
2022 Jan;23(1):81. PMID: 34934450 -
bioRxiv
2025 Nov 3:2025.10.31.685966. PMID: 41279778 -
bioRxiv
PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]2024 Nov 6:2024.11.04.621884. PMID: 39574568 -
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Solvente y solubilidad
DMSO : 50 mg/mL (131.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (13.18 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (13.18 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
MOLM-16 cells, purchased from DSMZ and cultured in RPMI containing 10% fetal bovine serum (FBS) and 1% L-glutamine, are plated at 20,000 cells per well in 96 well plates overnight. Cells are treated for 72 hours with compound or control vehicle (dimethyl sulfoxide) and cell viability is measured after the addition of Cell Titer-Blue for 4 hours at 37°C and reading of fluorescence on a Tecan Infinite® 200. The GI50 is determined by calculating growth at each dose relative to vehicle treated cells and cell viability at the time of treatment.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Dakin LA, et al. 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. 2012 Jul 15;22(14):4599-604. [Content Brief]
[2]. Kreuz S, et al. Loss of PIM2 enhances the anti-proliferative effect of the pan-PIM kinase inhibitor AZD1208 in non-Hodgkin lymphomas. Mol Cancer. 2015 Dec 8;14:205. [Content Brief]
[3]. Harada M, et al. The novel combination of dual mTOR inhibitor AZD2014 and pan-PIM inhibitor AZD1208 inhibits growth in acute myeloid leukemia via HSF pathway suppression. Oncotarget. 2015 Nov 10;6(35):37930-47. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6352 mL | 13.1759 mL | 26.3518 mL | 65.8796 mL |
| 5 mM | 0.5270 mL | 2.6352 mL | 5.2704 mL | 13.1759 mL | |
| 10 mM | 0.2635 mL | 1.3176 mL | 2.6352 mL | 6.5880 mL | |
| 15 mM | 0.1757 mL | 0.8784 mL | 1.7568 mL | 4.3920 mL | |
| 20 mM | 0.1318 mL | 0.6588 mL | 1.3176 mL | 3.2940 mL | |
| 25 mM | 0.1054 mL | 0.5270 mL | 1.0541 mL | 2.6352 mL | |
| 30 mM | 0.0878 mL | 0.4392 mL | 0.8784 mL | 2.1960 mL | |
| 40 mM | 0.0659 mL | 0.3294 mL | 0.6588 mL | 1.6470 mL | |
| 50 mM | 0.0527 mL | 0.2635 mL | 0.5270 mL | 1.3176 mL | |
| 60 mM | 0.0439 mL | 0.2196 mL | 0.4392 mL | 1.0980 mL | |
| 80 mM | 0.0329 mL | 0.1647 mL | 0.3294 mL | 0.8235 mL | |
| 100 mM | 0.0264 mL | 0.1318 mL | 0.2635 mL | 0.6588 mL |
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