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Dot1L-IN-5
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Catalog No. T11084Cas No. 2565705-03-3
Dot1L-IN-5 is a potent inhibitor of the disruptor of telomeric silencing 1-like protein ( DOT1L ) with an IC 50 SPA DOT1L of 0.17 nM [1].
Dot1L-IN-5
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Catalog No. T11084Cas No. 2565705-03-3
Dot1L-IN-5 is a potent inhibitor of the disruptor of telomeric silencing 1-like protein ( DOT1L ) with an IC 50 SPA DOT1L of 0.17 nM [1].
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,218 | 6-8 weeks | 6-8 weeks | |
| 50 mg | $1,985 | 6-8 weeks | 6-8 weeks | |
| 100 mg | $2,997 | 6-8 weeks | 6-8 weeks |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Dot1L-IN-5 is a potent inhibitor of the disruptor of telomeric silencing 1-like protein ( DOT1L ) with an IC 50 SPA DOT1L of 0.17 nM [1]. |
| Targets&IC50 | DOT1L:0.17 nM |
| In vitro | Dot1L-IN-5 (Compound 11) was evaluated through cellular assays for its efficacy in inhibiting H3K79 dimethylation in HeLa cells (ED 50 H3K79me2 Elisa = 2.9 nM) and suppressing HOXA9 gene expression in Molm-13 cells (ED 50 HOXA9 RGA = 30 nM) [1]. |
| In vivo | Dot1L-IN-5 (Compound 11), administered subcutaneously at a dosage of 75 mg/kg once daily for 20 days to NOD-SCID mice harboring MV4-11 tumor xenografts, failed to inhibit tumor growth. Conversely, administering the same compound twice daily for the same duration resulted in a significant 73% inhibition of tumor growth. Both administration schedules markedly reduced the global H3K79 dimethylation level in the tumor; however, the twice-daily regimen was notably more effective in decreasing the mRNA expression of the target genes HOXA9 and MEIS1. |
| Molecular Weight | 592.96 |
| Formula | C23H19ClF2N8O5S |
| Cas No. | 2565705-03-3 |
| Smiles | COc1nc(N)nc(Nc2cc(ccc2N[C@@H](c2cccc3OC(F)(F)Oc23)c2ncccc2Cl)S(N)(=O)=O)n1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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