Talmapimod-SCIO-469-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETalmapimodCat. No.: HY-10406CAS No.: 309913-83-5Synonyms: SCIO-469分式: CHClFNO分量: 513作靶点: p38 MAPK作通路: MAPK/ERK Pathway储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (194.93 mM)*

2、means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.9493 mL 9.7466 mL 19.4932 mL5 mM 0.3899 mL 1.9493 mL 3.8986 mL10 mM 0.1949 mL 0.9747 mL 1.9493 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

3、，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: 2.5 mg/mL (4.87 mM); Suspended solution; Need ultrasonic2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.87 mM); Clear solution1/3 Master of Small M

4、olecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.87 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Talmapimod (SCIO-469)是p38 选择性的ATP竞争抑制剂，IC50 值是9 nM。IC50 & Target IC50: 9 nM (p38) 1.体外研究 Talmapimod (SCIO-469)decreased constitutive p38 MAPK phosphorylation of both 5

5、T2MM and 5T33MMcells. Talmapimod (SCIO-469) also inhibits secretion and expression of the osteoclast-activating factors IL-11, receptor activator of NF-B ligand, and macrophage inflammatory protein 1, and prevents humanosteoclast activationIn. It can also inhibit multiple myeloma growth and prevents

6、 bone disease in the 5T2MMand 5T33MM models.体内研究 Targeting p38 MAPK with Talmapimod (SCIO-469) decreases myeloma burden in addition to preventing thedevelopment of myeloma bone disease.PROTOCOLCell Assay 5TMM cells (0.5 106/mL) were pretreated with different concentrations of Talmapimod (SCIO-469) i

7、nserum-free medium and then placed in the lower compartment of a Transwell system. Syngeneic bonemarrow stromal cells were seeded into the Transwell itself. After 18 h, the 5TMM cells were collected fromthe lower compartment and stained for active caspase-3 with a FITC-labeled antibody according tom

8、anufacturers instructionsMCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Animal injection 1Administration 1 For studies of the effect of Talmapimod (SCIO-469) on myeloma development, three groups of male mice (n= 12) were injected i.v. with 0.5 1

9、06 5T33MM cells. Mice were left untreated (naive) or, if injected withtumor cells, treated from the time of tumor cells injection with either Talmapimod (SCIO-469) (150 or 450mg/kg powder diet continuously available for the mice) or a vehicle (PBS) until the first mice showed signs ofmorbidity (at 3

10、.7 weeks).MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Hideshima T e

11、t al. p38 MAPK inhibition enhances PS-341 (bortezomib)-induced cytotoxicity against multiple myeloma cells. Oncogene.2004 Nov 18, 23(54), 8766-76.2. Vanderkerken K et al. Inhibition of p38alpha mitogen-activated protein kinase prevents the development of osteolytic bonedisease,reduces tumor burden, and increases survival in murine models of multiple myeloma. Vanderkerken K et al.McePdfHeightCaution: Product has