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SGI-1776 free base Sale

(Synonyms: SGI1776,SGI 1776) 目录号 : GC16497

A potent inhibitor of Pim kinases

SGI-1776 free base Chemical Structure

Cas No.:1025065-69-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥693.00
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5mg
¥641.00
现货
10mg
¥1,323.00
现货
50mg
¥3,213.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment: [1]

Cell lines

Primary lymphocytes from patients with CLL

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

10 μM, 24 hours

Applications

In vitro incubation of primary CLL cells with 1, 3, and 10 μM SGI-1776 for 24 hours resulted in an average increase in apoptosis of 10%, 22%, and 38%, respectively, compared with untreated cells. Incubation of CLL cells with SGI-1776 for 48 or 72 hours further increased the percentage of apoptotic cells.

Animal experiment: [2]

Animal models

Female BALB/c nude mice bearing 786-O or Caki-1 xenografts

Dosage form

Oral administration, 200 mg/kg, once every 5 days, for 3 weeks

Applications

Treatment with SGI-1776 resulted in a significant decrease in mean tumor volume in both xenograft models compared with the vehicle-treated controls. Besides that, SGI-1776 induced a reduction in Bad phosphorylation without altering total Bad protein levels. It also induced moderate levels of apoptosis.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Chen L S, Redkar S, Bearss D, et al. Pim kinase inhibitor, SGI-1776, induces apoptosis in chronic lymphocytic leukemia cells. Blood, 2009, 114(19): 4150-4157.

[2] Mahalingam D, Espitia C M, Medina E C, et al. Targeting PIM kinase enhances the activity of sunitinib in renal cell carcinoma. British journal of cancer, 2011, 105(10): 1563-1573.

产品描述

SGI-1776 free base, N-((1-methylpiperidin-4-yl)methyl)-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-amine, is a potent ATP-competitive inhibitor of the serine/threonine family of Pim kinase, an enzyme regulating cell survival. Through extensive biomedical characterization, SGI-1776 exhibits specificity to the three isoforms of the Pim family, including Pim-1, Pim-2, and Pim-3. According to preliminary results from studies treating prostate cancer cells, SGI-1776 dose-dependently reduces phosphorylation of known Pim kinase substrates involved in cell cycle progression and apotosis (p21Cip1/WAF1 and Bad), compromises overall cell viability by inducing G1 cell cycle arrest and triggering apoptosis, and reduces cell viability in a multidrug resistance 1 (MDR1) protein based taxane-refractory prostate cancer cell line.

Reference

[1].Shannon M. Mumenthaler, Patricia Y.B. Ng, Amanda Hodge, Davide Bearss, Gregory Berk, Sarath Kanekal, Sanjeev Redkar, Pietro Taverna, Davide B. Agus, and Anjali Jain. Pharmacological inhibition of Pim kinases alters prostate cancer cell growth and resensitizes chemoresistant cells to taxanes. Mol Cancer Ther. 2009; 8(10): 2882-2893
[2].Lisa S. Chen, S anjeev Redkar, David Bearss, William G. Wierda and Varsha Gandhi. Pim kinase inhibitor, SGI-1776, induces apoptosis in CLL lymphocytes. Blood. 2009; 114(19): 4150-4157

Chemical Properties

Cas No. 1025065-69-3 SDF
别名 SGI1776,SGI 1776
化学名 N-[(1-methylpiperidin-4-yl)methyl]-3-[3-(trifluoromethoxy)phenyl]imidazo[1,2-b]pyridazin-6-amine
Canonical SMILES CN1CCC(CC1)CNC2=NN3C(=NC=C3C4=CC(=CC=C4)OC(F)(F)F)C=C2
分子式 C20H22F3N5O 分子量 405.42
溶解度 ≥ 40.5 mg/mL in DMSO, ≥ 101 mg/mL in EtOH 储存条件 Store at -20°C
General tips 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.4666 mL 12.3329 mL 24.6658 mL
5 mM 0.4933 mL 2.4666 mL 4.9332 mL
10 mM 0.2467 mL 1.2333 mL 2.4666 mL
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