Wortmannin-SL-2052-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEWortmanninCat. No.: HY-10197CAS No.: 19545-26-7Synonyms: SL-2052; KY-12420分式: CHO分量: 428.43作靶点: PI3K; ATM/ATR; DNA-PK; Polo-like Kinase (PLK)作通路: PI3K/Akt/mTOR; Cell Cycle/DNA Damage储存式: Powder -20C 3 years4C 2 yearsIn solvent -

2、80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (116.71 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3341 mL 11.6705 mL 23.3410 mL5 mM 0.4668 mL 2.3341 mL 4.6682 mL10 mM 0.2334 mL 1.1671 mL 2.3341 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，并请注意储备液的保存式和期限。体内实验

3、请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.85 mM); Suspended solution; Need ultrasonic2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Sol

4、ubility: 2.08 mg/mL (4.85 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.85 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Wortmannin种多靶点抑制剂。Wortmannin 抑制 PI3K 1，MLCK 1，DNA-PK 2，ATM 2，ATR 2和 Polo-like kinase 3 (Plk3 3)，IC50

5、 分别为 3 nM，200 nM，16 nM，150 nM，1.8 M 和 48 nM。IC50 & Target PI3K DNA-PK PLK3 ATM3 nM (IC50) 16 nM (IC50) 48 nM (IC50) 150 nM (IC50)ATR MLCK1.8 M (IC50) 200 nM (IC50)体外研究 Wortmannin (0-100 nM; 24-72 hours) inhibits the proliferation of K562 cells in a time- and dose-dependentmanner. The IC50 values at

6、24 hour, 48 hour, and 72 hour are 250.10 nM, 12.50.08 nM, and 6.250.11nM, respectively 4.Cell Proliferation Assay 4Cell Line: K562 cellsConcentration: 0, 6.25, 12.5, 25, 50 and 100 nMIncubation Time: 0, 24, 48 and 72 hoursResult: Inhibited the K562 cells proliferation. The IC50 value at 24 hour, 48

7、hour, and 72 hourwas 250.10 nM, 12.50.08 nM, and 6.250.11 nM.体内研究Wortmannin (oral gavage; daily; in Scid mice; one group of eight mice is dosed with Wortmannin 1 mg/kg forall 14 days. The second group of eight mice is dosed with Wortmannin 1.5 mg/kg for the first 5 days and thedose is decreased to 1

8、 mg/kg for the remaining treatment period) treatment significantly slower the growthrate of murine C3H mammary tumor and human MCF-7 breast cancer xenograft. A dose of 1 mg/kgWortmannin for 7 days decrease the tumor burdens in mice with established murine C3H mammary tumorsby 54% relative to control

9、s. Human MCF-7 breast cancer xenograft burdens are decreased by 97% relativeto controls after 14 days of 1 mg/kg Wortmannin beginning 1 day after tumor implantation 5.Animal Model: Scid mice with the murine C3H mammary tumor or human MCF-7 breast cancerxenograft 5Dosage: 1 mg/kg and 1.5 mg/kgAdminis

10、tration: Oral gavage; daily; one group 1 mg/kg for 14 days; second group 1.5 mg/kg for 5 daysthen 1.0 mg/kg for 9 days.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEResult: The growth rate of the treated tumors was significantly slower during drug administrationthan that of nontreated tumors.户使本产

11、品发表的科研献 Cell Mol Life Sci. 2018 Jul;75(14):2627-2641. Cell Death Dis. 2019 Aug. J Mol Med (Berl). 2019 Jun 14. Arthritis Res Ther. 2018 Feb 7;20(1):20. Oncol Rep. 2019 Jun 19.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Yano H, et al. Inhibition of histamine secretion by wor

12、tmannin through the blockade of phosphatidylinositol 3-kinase in RBL-2H3 cells. JBiol Chem. 1993 Dec 5;268(34):25846-56.2. Sarkaria JN, et al. Inhibition of phosphoinositide 3-kinase related kinases by the radiosensitizing agent wortmannin. Cancer Res. 1998Oct 1;58(19):4375-82.3. Liu Y, et al. Polo-

13、like kinases inhibited by wortmannin. Labeling site and downstream effects. J Biol Chem. 2007 Jan 26;282(4):2505-11.4. Wu Q, et al. Wortmannin inhibits K562 leukemic cells by regulating PI3k/Akt channel in vitro. J Huazhong Univ Sci Technolog Med Sci.2009 Aug;29(4):451-6.5. Lemke LE, et al. Wortmannin inhibits the growth of mammary tumors despite the existence of a novel wortmannin-insensitivephosphatidylinositol-3-kinase. Cancer Chemother Pharmacol. 1999;44(6):491-