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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

Dot1L-IN-5

😃Good
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 SizePriceAvailabilityQuantity
25 mg$1,2186-8 weeks
50 mg$1,9856-8 weeks
100 mg$2,9976-8 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
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.
Chemical Properties
Molecular Weight592.96
FormulaC23H19ClF2N8O5S
Cas No.2565705-03-3
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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