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SGI-1776 free base

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Chemical Structure| 1025065-69-3 同义名 : SGI-1776;Pim-Kinase Inhibitor IX
CAS号 : 1025065-69-3
货号 : A290934
分子式 : C20H22F3N5O
纯度 : 99+%
分子量 : 405.417
MDL号 : MFCD16659064
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(295.99 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：

IP 2% DMSO+2% Tween80+40% PEG300+water 8 mg/mL clear

PO 0.5% CMC-Na 19 mg/mL suspension

生物活性
靶点

  • Pim3

    Pim3, IC50:69 nM

  • Pim1

    Pim1, IC50:7 nM

  • Pim2

    Pim2, IC50:363 nM
描述 Pim (provirus integration site for Moloney murine leukemia virus) family proteins are highly conserved serine/threonine kinases implicated in transcription, translation, cell cycle, survival, and drug resistance through the numerous targets. SGI-1776 is a dual Pim/FLT3 with IC50 values of 7nM, 363nM, 69nM and 44nM for Pim-1, Pim-2, Pim-3 (measurd by Kinase assays) and FLT3, respectively. Treatment with SGI-1776 at concentration<10μM caused decreased of p-H3-S10, p-cMyc-S62, p-BAD-S112, p-4E-BP1-Thr37/46, Mcl-1, as well as increased p27 in AML cell line MV-4-11. However, the decreased p-Bad-S112 and p-H3-S10 by SGI-1776 treatment were not observed in CLL lines, suggesting an alternative mechanism in different type of cells[1][2]. Incubation with 1, 3, and 10μM SGI-1776 for 24h resulted in an average increase in apoptosis of 10%, 22%, and 38% in CLL lymphocytes, mechanism of which may involved Mcl-1 reduction[1]. Also dose-dependent induction of cell death and reduction of clonogenic survival by SGI-1776<10μM can be observed in AML cell lines. Oral treatment with SGI-1776 at dose of 75mg/kg, QD, 5 days per week, for 3 weeks or 200mg/kg twice a week for 3 weeks could significantly reduce tumor growth in mice bearing MV-4-11 tumors[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
CHO cells Function assay Inhibition of human ERG expressed in CHO cells by automated patch clamp method, IC50=1 μM 25589932
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.47mL

0.49mL

0.25mL

12.33mL

2.47mL

1.23mL

24.67mL

4.93mL

2.47mL
参考文献

[1]Chen LS, Redkar S, et al. Mechanisms of cytotoxicity to Pim kinase inhibitor, SGI-1776, in acute myeloid leukemia. Blood. 2011 Jul 21;118(3):693-702.

[2]Chen LS, Redkar S, et al. Pim kinase inhibitor, SGI-1776, induces apoptosis in chronic lymphocytic leukemia cells. Blood. 2009 Nov 5;114(19):4150-7.