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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 | Availability | Quantity |
|---|---|---|---|
| 25 mg | $1,218 | 6-8 weeks | |
| 50 mg | $1,985 | 6-8 weeks | |
| 100 mg | $2,997 | 6-8 weeks |
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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.
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Product Introduction
Bioactivity
Chemical Properties
| 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 |
| Relative Density. | no data available |
Storage & Solubility Information
| 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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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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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