Dot1L-IN-5

Dot1L-IN-5

D646409-5mg

5mg

≥98%

-20°C储存

超低温冰袋运输

Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein ( DOT1L ) inhibitor with an IC 50 of 0.17 nM In Vitro Dot1L-IN-5 (Compound 11) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED 50 H3K79me2 Elisa =2.9 nM) and HOXA9 gene expression in Molm-13 cells (ED 50 HOXA9 RGA =30 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NOD-SCID mice bearing subcutaneous MV4-11 tumor xenografts 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. Form:Solid IC50& Target:DOT1L 0.17 nM (IC 50 )

Dot1L-IN-5 是一种强效的端粒沉默 1 类蛋白（DOT1L）抑制剂，其 IC 50 为 0.17 nM。

2565705-03-3

C23H19ClF2N8O5S

592.96 g/mol

O=S(C1=CC=C(N[C@H](C2=NC=CC=C2Cl)C3=C4OC(F)(F)OC4=CC=C3)C(NC5=NC(N)=NC(OC)=N5)=C1)(N)=O

DMSO : 250 mg/mL (421.61 mM; Need ultrasonic)