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现货,Dovitinib Dilactic acid (TKI258 Dilactic acid),selleck,美国进口, Flt YZ剂,CAS号: 852433-84-2,目录号 S1018

产品信息
  • 规格: 48T 产品价格: ¥3213
    规格: 10mg 产品价格: ¥3213
    S1018 Dovitinib Dilactic acid (TKI258 Dilactic acid)
    信号转导通路:  受体酪氨酸激酶(RTK) >> Flt >> Flt YZ剂 >> 
    技术数据:
    分子量(MW): 572.59
    化学式:

    C21H21FN6O.2C3H6O3

    溶解度: DMSO ≥115mg/mL   Water ≥115mg/mL   Ethanol <1mg/mL
    纯度: >99%
    稳定性: at -20℃ 2 years
    CAS号: 852433-84-2
    生物活性

     

    Dovitinib是多靶点酪氨酸激酶YZ剂,作用于FLT3和c-KIT时IC50分别为1,2 nM。Dovitinib有效YZFGFR1/3和VEFFR1-2,IC50为8-13 nM。Dovitinib对InsR, EGFR, c-Met, EphrinA2, Tie2, IGFR1,和HER2YZ效果不大。Dovitinib作用于FGF刺激的野生型B9细胞和F384L突变型B9细胞的生长显示出强细胞毒性,IC50为25 nM。然而,Dovitinib作用于MINV突变型B9细胞显示出低细胞毒性。DovitinibYZ下游ERK1/2的磷酸化作用。 [1] Dovitinib作用于MV4;11 (FLT-3 ITD突变型)时比作用于RS4;11 (FLT-3野生型)显示出更高的抗恶性细胞增生的能力。[2] 另一方面,Dovitinib也选择性地YZFGFR1癌基因配体2-FGFR-阳性的KG1和KG1A 细胞系,这些细胞系有FGFR1癌基因配体2-FGFR1聚合基因。另外,DovitinibYZ8p11增殖综合征(EMS)病人的原代细胞生长。[3] 在KMS-11移植鼠模型中,按鼠体重,每千克处理60 mg Dovitinib,导致FGFR3的衰退,结果肿瘤生长YZ率达到94%。[1]在SCID-NOD 鼠中,Dovitinib作用于MV4;11肿瘤时显示出强的活性。[2]Dovitinib也有效YZ能激活FGFR3的KMS-11肿瘤。[4]DovitinibZL实体瘤和子宫内膜癌目前已经处于二期临床实验阶段。DovitinibZ初是由Chiron研究的,后来是由Novartis在研究。

     

    参考文献

    [1] Trudel S, et al, Blood, 2005, 105 (7), 2941-2948.
    [2] Lopes De Menezes DE, et al, Clin Cancer Res, 2005, 11 (14), 5281-5291.
    [3] Chase A, et al, Blood, 2007, 110 (10), 3729-3734.
    [4] Xin X, et al, Clin Cancer Res, 2006, 12 (16), 4908-4915.

    客户反馈数据

    RT112 cells were exposed to PD173074 (PD) (500 nM) for 0–24 h, TKI-258 (TK) (500 nM) or SU5402 (SU) (5 mM) for 1 h. Cells were lysed, FGFR3 was immunoprecipitated (immunoprecipitated, IP) and blots (immunoblot, IB) were probed for phospho-tyrosine and reprobed for FGFR3 or probed for phospho-ERK and reprobed for total ERK.

     

     

    Cells were exposed to PD173074 or TKI-258 (500 nM) for 24 h. Cell cycle profile was analysed using the Guava Easycyte Plus flow cytometry system.

     

     

    In vitro assays on CUX1-FGFR1-expressing Ba/F3 cells. a. IL-3 deprivation of Ba/F3 cells transduced with CUX1-FGFR1 resulted in transformation to growth factor independent growth. The mean growth ± SEM of three separate measurements over four consecutive days is presented. b. The dose-response curves of CUX1-FGFR1-transduced Ba/F3 cells, treated with TKI258 and PKC412 for 48 hours in the absence or presence of IL-3 (2ng/ml) are presented. Points represent the average results of two experiments done in triplicate plotted with the curve-fitting GraphPad Prism 5 software; bars, SD. The calculated IC50 for each inhibitor is indicated. c. Western blot analyses of CUX1-FGFR1-transformed Ba/F3 cells after treatment with PKC412 and TKI258. Phosphorylation of CUX1-FGFR1 and its downstream effectors STAT5 and RPS6K decreased with increasing inhibitor concentrations. Expression of total CUX1-FGFR1, STAT5 and RPS6K remained unaffected. d. Effect of PKC412 and TKI258 on apoptosis of CUX1-FGFR1-expressing Ba/F3 cells after treatment for 48 hours. The percentage of apoptotic plus necrotic CUX1-FGFR1-transduced Ba/F3 cells is indicated.

     

     

    Ba/F3 cell lines expressing the recombinant TEL/kinase domain fusion protein for FGFR1-4 .Cells were grown in RPMI 1640 containing 10% FBS and 500 ng/mL puromycin. The parental Ba/F3 cell line transduced with an empty vector was grown in 10 ng/mL IL-3 (R & D systems). Cell viability was assessed at 72 hours using the Cell Titer 96 Aqueous One Solution (Promega). Data were plotted as percent viability relative to vehicle-treated cells and are shown as mean (± SD) from 3 experiments.

     

     

    如果需要长期保存,请于零下二十度低温保存。
    禁止用于人体及ZL!

    特定的存储和包装每个产品的信息在产品说明书上都有注明 。大多数Selleck产品,在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同,大多数建议储存在-20 ° C ,抗体及蛋白等产品建议-60℃。YZ剂属于化学试剂,可在常温下运输储存两周左右。即使如此,我们保证产品的出货量将保持产品质量的条件下,一般都会放入冰袋。望阁下收到产品后,请按照产品数据表建议适当存储。

    温馨提示:不可用于临床ZL。
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