1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects.
IC50&Target
IC50: 12 nM (DPP8), 84 nM (DPP9)
体外研究
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.
1G244 (50 μM; 0-48 hours; MM.1 S cells) treatment induces apoptosis, as cleaved forms of both caspase-3 and PARP are detected.
Cell Viability Assay
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.
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.
Animal Model:
NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21 g) injected with MM.1 S cells
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.
分子式
C29H30F2N4O2
分子量
504.57
CAS号
847928-32-9
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
浓度溶剂体积质量
1 mg
5 mg
10 mg
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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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: