体外研究(In Vitro)
SGC0946 (0-100 μM; 4 days) inhibits DOT1L with IC50 of 2.65 nM in A431 cells[1].
SGC0946 (1, 5 μM; 14 days) displays selective reduction of cell viability in an experimental leukaemia model derived from human cord blood cells (transformed with the MLL-AF9 fusion oncogene)[1].
SGC0946 (1 μM; 3-7 days) shows time- and dose-dependent reductions in the H3K79me2 mark in the Molm13 MLL cell line that has the MLL/AF9 translocation[1].
SGC0946 (1 μM, 7 days) effectively inhibits MLL target genes, HOXA9 and Meis1[1].
SGC0946 (0.2, 2, or 20 μM; 12 days) reduces proliferation and survival of ovarian cancer cells by inhibiting DOT1L enzymatic activity[2].
SGC0946 (10 μM; 12 days) induces G1 phase arrest by blocking DOT1L in SK-OV-3 and TOV21G cells[2].
体内研究(In Vivo)
SGC0946 (10 mg/kg; i.p.; twice a week for 6 weeks) significantly suppresses tumor progression in a mouse orthotopic xenograft ovarian cancer model and also inhibits DOT1L enzymatic activity and levels of H3K79me2,CDK6, and cyclin D3 in the tumors[2]
分子量
618.57
性状
Solid
Formula
C28H40BrN7O4
CAS 号
1561178-17-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro:
DMSO : 50 mg/mL (80.83 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 1.6166 mL 8.0832 mL 16.1663 mL
5 mM 0.3233 mL 1.6166 mL 3.2333 mL
10 mM 0.1617 mL 0.8083 mL 1.6166 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: