1G244 是一种有效的DPP8/9抑制剂,IC50分别为 12 nM 和 84 nM,但不抑制 DPPIV 和 DPPII。1G244 可诱导多发性骨髓瘤细胞凋亡,并具有抗骨髓瘤作用。
生物活性 | 1G244 is a potentDPP8/9inhibitor withIC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 inducesapoptosisin multiple myeloma cells and has anti-myeloma effects[1][2]. |
IC50& Target | IC50: 12 nM (DPP8), 84 nM (DPP9)[2] |
体外研究 (In Vitro) | 1G244 (0-100 μM; 72 hours; Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells) treatment dose-dependently decreases viable cell number of five multiple myeloma cell lines[1]. 1G244 (50 μM; 0-48 hours; MM.1 S cells) treatment induces apoptosis, as cleaved forms of both caspase-3 and PARP are detected[1].
Cell Viability Assay[1] Cell Line: | Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells | Concentration: | 0 μM, 1 μM, 5 μM, 10 μM, 50 μM, or 100 μM | Incubation Time: | 72 hours | Result: | Dose-dependently decreased viable cell number of five multiple myeloma cell lines. |
Western Blot Analysis[1] Cell Line: | MM.1 S cells | Concentration: | 50 μM | Incubation Time: | 0 hour, 3 hours, 6 hours, 12 hours, 24 hours, 48 hours | Result: | Decreased caspase-3 and PARP protein. |
|
体内研究 (In Vivo) | 1G244 (30 mg/kg; subcutaneous injection; once-a-week; for 3 weeks; NOG female mice) treatment apparently suppresses the subcutaneous growth of MM.1 S cells in murine xenograft model[1].
Animal Model: | NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21 g) injected with MM.1 S cells[1] | Dosage: | 30 mg/kg | Administration: | Subcutaneous injection; once-a-week; for 3 weeks | Result: | Apparently suppressed the subcutaneous growth of MM.1 S cells in murine xenograft model. |
|
分子量 | |
性状 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: DMSO : 250 mg/mL(495.47 mM;Need ultrasonic) 配制储备液 1 mM | 1.9819 mL | 9.9094 mL | 19.8189 mL | 5 mM | 0.3964 mL | 1.9819 mL | 3.9638 mL | 10 mM | 0.1982 mL | 0.9909 mL | 1.9819 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.12 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.12 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
|