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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 |
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 | 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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