生物活性
SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.
体外研究(In Vitro)
SGI-1027 is a DNMT inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate. SGI-1027 shows an IC50 of 6 μM for DNMT1 (hemimethylated DNA). SGI-1027 (1, 2.5, or 5 µM) causes selective degradation of DNMT1 in several human cancer cell lines, but shows little or no cytotoxic effect on rat hepatoma cells, and does not induce apoptosis in rat hepatoma cells[1]. SGI-1027 shows an EC50 of 0.9 μM for hDNMT3A, and causes cytotoxicity on KG-1 cells, with an EC50 of 4.4 μM[2].
分子量
461.52
性状
Solid
Formula
C27H23N7O
CAS 号
1020149-73-8
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 : 27 mg/mL (58.50 mM; Need ultrasonic and warming)
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 2.1668 mL 10.8338 mL 21.6675 mL
5 mM 0.4334 mL 2.1668 mL 4.3335 mL
10 mM 0.2167 mL 1.0834 mL 2.1668 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: