LY2874455
作者：齊岳
發(fā)布時(shí)間：2023-08-28
09:00:57
點(diǎn)擊數(shù)：
產(chǎn)品名稱：LY2874455
產(chǎn)品描述：
| 產(chǎn)品描述 | LY2874455 has been used in trials studying the treatment of Advanced Cancer. |
| 靶點(diǎn)活性 | FGFR4:6 nM, FGFR3:6.4 nM, FGFR1:2.8 nM, FGFR2:2.6 nM, VEGFR2:7 nM |
| 體外活性 | 在攜帶RT-112,OPM-2（DSMZ）,SNU-16或NCI-H460異種移植物的小鼠中,LY2874455（3 mg/kg,口服）導(dǎo)致腫瘤生長(zhǎng)的劑量依賴性抑制.LY2874455在小鼠心臟組織中,表現(xiàn)出對(duì)FGF誘導(dǎo)的Erk磷酸化的有效抑制,TED50和TED90值分別為1.3 和 3.2 mg/kg. |
| 體內(nèi)活性 | LY2874455在KMS-11,OPM-2,SNU-16和KATO-III細(xì)胞中顯示FGFR依賴性抗增殖作用。在RT-112細(xì)胞,HUVECs,KATO-III細(xì)胞和SNU-16細(xì)胞中,LY2874455抑制FGF/FGFR介導(dǎo)的信號(hào)傳導(dǎo)活性。 |
| 激酶實(shí)驗(yàn) | Biochemical filter-binding assays for detection of FGFR phosphorylation activities : Reaction mixtures contains 8 mM Tris-HCl (pH 7.5), 10 mmol/L HEPES, 5 mM dithiothreitol, 10 μM ATP, 0.5 μCi 33P-ATP, 10 mM MnCl2, 150 mM NaCl, 0.01% Triton X-100, 4% dimethyl sulfoxide, 0.05 mg/mL poly(Glu:Tyr) (4:1, average molecular weight of 20–50 kDa), and 7.5, 7.5, and 16 ng of FGFR1, FGFR3, and FGFR4, respectively, and are incubated at room temperature for 30 minutes followed by termination with 10% H3PO4. The reaction mixtures are transferred to 96-well MAFB filter plates that are washed 3 times with 0.5% H3PO4. After air-drying, the plates are read with a Trilux reader. |
| 細(xì)胞實(shí)驗(yàn) | Cells (2,000 per well) are first grown in RPMI for 6 hours and treated with LY2874455 at 37 ℃ for 3 days. The cells are stained at 37℃ for 4 hours and then solubilized at 37℃ for 1 hour. Finally, the plate is read at 570 nm using a plate reader (Spectra Max Gemini XS). (Only for Reference) |
| 別名 | LY-2874455, LY 2874455 |
| 分子量 | 444.32 |
| 分子式 | C21H19Cl2N5O2 |
| CAS No. | 1254473-64-7 |
存儲(chǔ)
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 82 mg/mL (184.6 mM)
Ethanol: 53 mg/mL (119.3 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷(xiāo)售等。涉及產(chǎn)品為通用試劑的分銷(xiāo)、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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