S80001 |
KW-2449 |
源葉(MedMol) | 99% |
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- 產(chǎn)品描述: KW-2449是一種多靶點(diǎn)抑制劑,最有效作用于Flt3,IC50為6.6 nM,作用于Flt3, Bcr-Abl和Aurora A適度有效;對(duì)PDGFRβ, IGF-1R, EGFR沒(méi)有抑制效果。Phase 1
- 靶點(diǎn): Apoptosis;FGFR;FLT;JAK;Bcr-Abl;Src;c-Kit;AuroraKinase
- 體外研究:
KW-2449 shows growth inhibitory activities against FLT3/ITD-, FLT3/D835Y-, and wt-FLT3/FL-expressing 32D cells, MOLM-13 and MV4;11 with GI50 values of 0.024, 0.046, 0.014, 0.024, and 0.011 μM, respectively. KW-2449 suppresses the phosphorylations of FLT3 (P-FLT3) and its downstream molecule phospho-STAT5 (P-STAT5) in MOLM-13 cells in a dose-dependent manner. KW-2449 increases the percentage of cells in the G1 phase of the cell cycle and reciprocally reduced the percentage of cells in the S phase, resulting in the increase of apoptotic cell population.
- 體內(nèi)研究:
KW-2449口服處理給藥MOLM-13移植瘤模型,處理14天,具有顯著的抗癌效果,這種作用存在劑量依賴性
- 細(xì)胞實(shí)驗(yàn): Cell lines: MOLM-13和 RS4;11細(xì)胞 Concentrations: 33nM, 75nM, 0.1μM, 0.3μM ,0.15μM Incubation Time: 24, 48, 和72小時(shí) Method: 與KW-2449在37oC下溫育72小時(shí)后,通過(guò)3′-[1-(羰基苯胺)-3, 4-四氮唑]- 雙(4-甲氧基-6-硝基) 苯磺酸鈉水合物法測(cè)定細(xì)胞活力使用細(xì)胞增殖試劑盒 II測(cè)定存活細(xì)胞數(shù)。為了分析細(xì)胞周期,使用 KW-2449處理 MOLM-13 和 RS4; 11細(xì)胞。在37oC下溫育24,48,和72小時(shí)后,分析 DNA含量。使用KW-2449或Imatinib處理24小時(shí)后,分析K562, TCC-Y, 和 TCC/Ysr細(xì)胞周期分布
- 動(dòng)物實(shí)驗(yàn): Animal Models: CBySmn.CB17-Prkdsscid/J (BALB/C) 小鼠, 溶于100 μL PBS的2×106 BV173/E255K/Luc cl4 細(xì)胞注射到鼠尾部靜脈 Dosages: 32 mg/kg/day, 5 days/week Administration: 口服處理
- 參考文獻(xiàn):
1. Shiotsu Y, et al. KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation. Blood, 2009, 114(8), 1607-17. 2. Pratz KW, et al. A pharmacodynamic study of the FLT3 inhibitor KW-2449 yields insight into the basis for clinical response. Blood, 2009, 113(17), 3938-46. 3. Nguyen T, et al. HDAC inhibitors potentiate the activity of the BCR/ABL kinase inhibitor KW-2449 in imatinib-sensitive or -resistant BCR/ABL+ leukemia cells in vitro and in vivo. Clin Cancer Res, 2011, 17(10), 3219-32.
- 溶解性: Soluble in DMSO、Ethanol
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 3.008 ml 15.042 ml 30.084 ml 5 mM 0.602 ml 3.008 ml 6.017 ml 10 mM 0.301 ml 1.504 ml 3.008 ml 50 mM 0.06 ml 0.301 ml 0.602 ml
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輸入產(chǎn)品批號(hào):
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)