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CAS No.: 1025065-69-3

SGI-1776 游离碱 Catalog No. CSN17161

Synonyms: Pim-Kinase Inhibitor IX;SGI-1776 Free Base

SGI-1776 free base is an ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 FLT3

IC50:44nM Pim1

IC50:7nM Pim2

IC50:363nM Pim3

IC50:69nM
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
Cell Data
Cell Lines Concentration Assay Type Time Activity Description Data Sources
CHO cells - Function assay - Inhibition of human ERG expressed in CHO cells by automated patch clamp method, IC50=1 μM 25589932
动物研究
剂量
Mice: 50 mg/kg - 200 mg/kg^[2] (p.o.)

给药途径
p.o.
临床研究

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
CHO cells	-	Function assay	-	Inhibition of human ERG expressed in CHO cells by automated patch clamp method, IC50=1 μM	25589932

动物研究
剂量	Mice: 50 mg/kg - 200 mg/kg^[2] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01239108	Relapsed/Refractory Leukemias	Phase 1	Withdrawn(The dose limiting to... more >>xicity of cardiac QTc prolongation was identified and demonstrated unsafe to continue clinical development of this molecule.) Collapse <<	April 2012	United States, Texas ... more >> MD Anderson Cancer Center Houston, Texas, United States Collapse <<
NCT00848601	Prostate Cancer ... more >> Non-Hodgkins Lymphoma Collapse <<	Phase 1	Terminated(The dose limiting t... more >>oxicity of cardiac QTc prolongation was identifiedin the phase 1 study in patients with refractory prostate and lymphoma) Collapse <<	-	United States, California ... more >> UCLA Los Angeles, California, United States, 90095-1678 United States, Texas Cancer Therapy Research Center San Antonio, Texas, United States, 78229 United Kingdom Royal Marsden Hospital Sutton, England, United Kingdom, SM2 5PT Collapse <<

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4666 mL
- 12.3330 mL
- 24.6660 mL
- 5 mM
- 0.4933 mL
- 2.4666 mL
- 4.9332 mL
- 10 mM
- 0.2467 mL
- 1.2333 mL
- 2.4666 mL

技术信息

CAS号

1025065-69-3

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H22F3N5O

运输

蓝冰

分子量

405.42

别名

Pim-Kinase Inhibitor IX;SGI-1776 Free Base

溶解度

DMSO	500.0 mg/mL (1233.3 mM) warming
Water	insoluble

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

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靶点	Description	IC50
FLT3		IC50:44nM
Pim1		IC50:7nM
Pim2		IC50:363nM
Pim3		IC50:69nM

SGI-1776 游离碱 Catalog No. CSN17161

靶点选择性

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