Dot1L-IN-5 是一种有效的类端粒沉默干扰体 1 (DOT1L) 抑制剂，IC50 SPA DOT1L 为 0.17 nM。
| Cas No. | 2565705-03-3 |
| 分子式 | C23H19ClF2N8O5S |
| 分子量 | 592.96 |
| 溶解度 | DMSO : 250 mg/mL (421.61 mM; Need ultrasonic) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with anIC50 SPA DOT1Lof 0.17 nM[1]. Dot1L-IN-5 (Compound 11) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED50 H3K79me2 Elisa=2.9 nM) and HOXA9 gene expression in Molm-13 cells (ED50 HOXA9 RGA=30 nM)[1]. Dot1L-IN-5 (Compound 11; subcutaneous injection; at 75 mg/kg once daily for 20 days) does not lead to tumor growth inhibition in NOD-SCID mice. Dot1L-IN-5 (subcutaneous injection; at 75 mg/kg twice daily for 20 days) leads 73% growth inhibition[1].
While both treatment regimens result in very strong inhibition of global H3K79 dimethylation level in tumor, the efficacious regimen is superior in reducing the mRNA expression of the target genes HOXA9 and MEIS1[1]. | Animal Model: | NOD-SCID mice bearing subcutaneous MV4-11 tumor xenografts[1] | | Dosage: | 75 mg/kg | | Administration: | Subcutaneous injection; at 75 mg/kg once or twice daily for 20 days | | Result: | Once daily administration did not lead to tumor growth inhibition, 73% growth inhibition was measured in the twice daily treated group. |
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