中文名稱:化合物 SB1317 | 英文名稱:SB1317 |
CAS:1204918-72-8 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
產(chǎn)品類別: 抑制劑 | |
貨號: T2653 |
Name | SB1317 |
Description | SB1317 (TG02) is a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3). |
Cell Research | SB1317 is prepared in DMSO and stored, and then diluted with appropriate medium before use[1]. All cell lines are obtained from the American Type Culture Collection and cultured. For proliferation assays in 96-well plates, 20 000 cells are seeded in 100 μL of medium and treated the following day with compounds (e.g., SB1317 ) (in triplicate) at concentrations up to 10 μM for 48 h. Cell viability is monitored using the CellTiter-96 Aqueous One solution cell proliferation assay. Dose-response curves are plotted to determine IC50 values for the compounds using the XL-fit software[1]. |
Kinase Assay | The recombinant enzymes (CDK2/cyclin A, JAK2, and FLT3) are used. All assays are carried out in 384-well white microtiter plates using the PKLight assay system. This assay platform is a luminometric assay for the detection of ATP in the reaction using a luciferase-coupled reaction. The compounds are tested at eight concentrations prepared from 3- or 4-fold serial dilution starting at 10 μM. For CDK2/cyclin A assay, the reaction mixture consisted of the following components in 25 μL of assay buffer (50 mM Hepes, pH 7.5, 10 mM MgCl2, 5 mM MnCl2, 5 mM BGP, 1 mM DTT, 0.1 mM sodium orthovanadate), 1.4 μg/mL of CDK2/cyclin A complex, 0.5 μM RbING substrate, and 0.5 μM ATP. The mixture is incubated at room temperature for 2 h. Then 13 μL of PKLight ATP detection reagent is added and the mixture is incubated for 10 min. Luminescence signals are detected on a multilabel plate reader. The analytical software Prism 5.0 is used to generate IC50 values from the data[1]. |
In vitro | SB1317是一種具有高度獨特的激酶抑制譜的化合物,能夠抑制一個由63個激酶組成的面板中的17種激酶,其中11種屬于CDK/JAK/FLT家族。其余的,包括Lck、Fyn、Fms、TYRO3、ERK5和p38δ,都與炎癥和增殖過程有關(guān)。在最高測試濃度25 μM時,人類CYP1A2、3A4、2C9和2C19同工酶未被SB1317抑制,但SB1317以IC50=0.95 μM抑制CYP2D6,接近于最大耐受劑量時觀察到的血漿Cmax。SB1317在HCT-116(IC50=0.079 μM)和HL-60(IC50=0.059 μM)細胞中抑制細胞增殖[1]。SB1317是一種新型的、小分子的強效CDK/JAK2/FLT3抑制劑,主要通過CYP3A4和CYP1A2在體外代謝。除CYP2D6(IC50=1 μM)外,SB1317不抑制任何主要的人類CYPs,并且在體外的人類肝細胞中不顯著誘導CYP1A和CYP3A4[2]。 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 10 mM |
Keywords | TG 02 | SB 1317 | SB1317 | TG-02 | SB-1317 |
Inhibitors Related | Tofacitinib Citrate | Sodium Oxamate | Gilteritinib | Ribociclib | CASIN | Sorafenib tosylate | Nintedanib | Sorafenib | Pexidartinib | Palbociclib | Ruxolitinib phosphate | Abemaciclib |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 566.265100萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學,分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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