AZD1208 hydrochloride |
| Katalog-Nr.GC35447 |
AZD1208-Hydrochlorid ist ein oral bioverfÜgbarer, hochselektiver PIM-Kinasen-Inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1621866-96-3
Sample solution is provided at 25 µL, 10mM.
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AZD1208 hydrochloride is a novel, orally bioavailable, highly selective PIM kinases inhibitor. PIM[1]
AZD1208 hydrochloride shows good antiproliferative activity in a megakaryoblastic leukemia cell line, MOLM-16, with GI50 values less than 100 nM[1]. AZD1208 hydrochloride (10 μM) inhibits the growth of Ramos cells, and at 1 μM, strongly inhibits PIM kinases in all cells at 1 μM. AZD1208 hydrochloride induces apoptosis, and PIM2 knockdown is mainly associated with an alteration of the cell cycle[2]. The combination of AZD1208 hydrochloride 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].
[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. [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. [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.
| Cas No. | 1621866-96-3 | SDF | |
| Canonical SMILES | O=C(NC/1=O)SC1=C/C2=C(N3C[C@H](N)CCC3)C(C4=CC=CC=C4)=CC=C2.[H]Cl | ||
| Formula | C21H22ClN3O2S | M.Wt | 415.94 |
| Löslichkeit | DMSO: 83.3 mg/mL (200.27 mM and warming) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4042 mL | 12.021 mL | 24.0419 mL |
| 5 mM | 0.4808 mL | 2.4042 mL | 4.8084 mL |
| 10 mM | 0.2404 mL | 1.2021 mL | 2.4042 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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