SC99

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Chemical Structure| 882290-02-0 同义名 : -
CAS号 : 882290-02-0
货号 : A1359457
分子式 : C15H8Cl2FN3O
纯度 : 99%+
分子量 : 336.148
MDL号 : MFCD00176649
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 85 mg/mL(252.86 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Signal transducer and activator of transcription 3 (STAT3) is an oncogenic transcription factor widely expressed in many tissues and plays an important role in regulating cellular activities. SC99 is a novel STAT3 inhibitor which could be developed as an anti-myeloma agent. In five MM cell lines with highly activated STAT3, SC99 (10 μM) decreased the p-STAT3 level but had no effects on total STAT3 expression. Moreover, SC99 suppressed STAT3 activation in a concentration- and time-dependent manner. In OPM2 cells, SC99 (0, 2.5, 5, 10 μM) inhibited JAK2 phosphorylation in a concentration-dependent manner. In OPM2 and RPMI-8226 cells, SC99 (0, 2.5, 5, 10, 20 μM; 24 hrs) suppressed the expression of cyclin D2 and E2F-1 in a concentration-dependent manner. Oral administration of SC99 led to marked decrease of tumor growth within 10 days at a daily dosage of 30 mg/kg[1].
作用机制 SC99 was well docked into the ATP-binding pocket of JAK2 in which SC99 formed strong and stable hydrogen bond with Leu932 of JAK2[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.97mL

0.59mL

0.30mL

14.87mL

2.97mL

1.49mL

29.75mL

5.95mL

2.97mL
参考文献

[1]Zhang Z, et al. A novel small molecule agent displays potent anti-myeloma activity by inhibiting the JAK2-STAT3 signaling pathway. Oncotarget. 2016 Feb 23;7(8):9296-308