AZD1208

目录号:S7104

AZD1208 Chemical Structure

Molecular Weight(MW): 379.48

AZD1208是一种有效的口服可利用的Pim kinase抑制剂,在无细胞试验中对Pim1, Pim2, and Pim3的IC50分别为0.4 nM,5 nM,和 1.9 nM。Phase 1。

规格 价格 库存 购买数量  
RMB 874.79 现货
RMB 3016.07 现货
RMB 6467.33 现货
有超大折扣

今日订购,明日送达,全国免运费!

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck该产品发表文献17篇:

客户使用该产品的6个实验数据:

  • Loss of proliferation in ATL-derived cell lines by the Pim-kinase inhibitor AZD1208 (D). Cell counts were repeated at least twice. Results represent the percentage of cells alive after 5 days of Pim inhibitor treatment, compared with 5 days treated with DMSO. For AZD1208, cells were treated with 0, 5, or 10 μM AZD1208. Normal PBMCs (n = 2) were used as a control. Western blots indicate loss of Pim1 targets, p-4EBP1 (Thr37/46), p-p70S6K (Thr389), and loss of pBad (Ser20) (negligible for Smi-4a) after 24 hours with 0, 5, or 10 μM AZD1208; or DMSO control.

    Blood, 2016, 127(20):2439-50.. AZD1208 purchased from Selleck.

  • Primary AML sample (AML#6) treated with the pan-Pim kinases inhibitors AZD1208 (1 μM) or LGB321 (1 μM). Western blots were done using RSK2, Pim2 and β-actin antibodies.

    Leukemia, 2018, 32(3):597-605. AZD1208 purchased from Selleck.

  • AZD1208-resistant cell lines demonstrate sustained mTOR signaling upon treatment. Cells were treated with 2 μmol/L AZD1208 for 0, 24, and 48 hours, followed by Western blot analysis (n = 3).

    Mol Cancer Ther, 2018, 17(4):849-857. AZD1208 purchased from Selleck.

  • (D) IC50 values calculated from cell viability assays of indicated cell lines, with the top concentration for PIM447 and AZD1208 being 10 μM. Shown is the mean of four replicates ± SEM. (E) IC50 values calculated from cell viability assays of indicated cell lines, with the top concentration for AEB071 being 10 μM and 1 μM for Ibrutinib. Shown is the mean of four replicates ± SEM. (F) ABC DLBCL cell lines, grouped based on drug sensitivity, with known somatic mutations.

    Oncotarget, 2016, 7(39):63362-63373. AZD1208 purchased from Selleck.

  • (D) HBL1 cells were plated in 0.9% MethoCult (1,000 cells/well) with vehicle, ibrutinib (100 or 1,000 nM), AZD-1208 (100 or 1,000 nM), or the combinations, and colony formation was scored after 7 days. Graphs represent quantifications of 3 wells, expressed as mean ± SD. (E) HBL1 tumor cells were implanted into CB17 SCID mice, and the indicated drugs were orally administered daily when the tumors reached 150 mm3. Tumors were measured twice a week. Significant tumor suppression was observed in the group treated with the ibrutinib/AZD-1208 combination compared with the vehicle-treated group (*P<0.01, repeated measures MANOVA-adjusted univariate F-test).

    Am J Cancer Res, 2016, 6(11):2489-2501. AZD1208 purchased from Selleck.

  • Effect of the Pim1 inhibitor AZD1208 on the expression of NFIL3 (at 24 h) and viability of eosinophils (at 48 h) stimulated with IL-5 and Dex. A) AZD1208 at a concentration specific for inhibition of Pim1 activity (1ng/ml) blocked upregulation of NFIL3 by IL-5 and Dex/IL-5 (24 h) without a significant effect on Pim1 expression. B) Inhibition of Pim1 activity by AZD1208 blocked the anti-apoptotic effect of IL-5 and restored the proapoptotic effect of Dex on activated eosinophils, * p<0.05 vs. control cells. The error bars represent the standard deviation of 4 experiments from 3 independent donors.

    Apoptosis, 2016, 21(4):421-31. AZD1208 purchased from Selleck.

产品安全说明书

Pim抑制剂选择性比较

生物活性

产品描述 AZD1208是一种有效的口服可利用的Pim kinase抑制剂,在无细胞试验中对Pim1, Pim2, and Pim3的IC50分别为0.4 nM,5 nM,和 1.9 nM。Phase 1。
特性 Pim激酶抑制剂的口服生物活性已经在I期临床试验中进行了测试,用于治疗晚期实体瘤和恶性淋巴瘤。
靶点
Pim1 [1]
(Cell-free assay)
Pim3 [1]
(Cell-free assay)
Pim2 [1]
(Cell-free assay)
0.4 nM 1.9 nM 5 nM
体外研究

AZD1208是一种可口服的,有效的高选择性Pim抑制剂,能够有效抑制三种亚型。AZD1208抑制几种与Pim-1表达水平,STAT5激活和蛋白酪氨酸激酶突变存在下相对应的AML细胞系的生长和敏感性。AZD1208引起培养基中MOLM-1细胞的细胞周期阻滞和凋亡。这伴随着BAD,4EBP1 和p70S6K磷酸化作用的剂量依赖性减少。此外,AZD1208有效抑制初级骨髓穿刺液中AML细胞的集落生长, 并下调Pim靶点的磷酸化作用。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLM16 cells M3rLW3Bzd2yrZnXyZZRqd25iYYPzZZk> MVi3NkBp MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2RTF2xOkBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XscEBVcXSncj3CcJVmKGG|c3H5MEBIUTVyPUCuNFIh|ryP NHi4VI0zOjd{N{[0NC=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cleaved PARP / Myc / p-PRAS40 / PRAS40 / p-S6 / p-4EBP1 / 4EBP1 / p-BAD / BAD; 

PubMed: 27270648     


AZD1208-resistant AML cell lines demonstrate sustained mTOR signaling upon treatment. Cells were treated for 4, 24, and 48 hours with 1 μM AZD1208 followed by western blot analysis (n = 3). 

p-MKK4 / p-p38 / p-MK2 / p-AKT ; 

PubMed: 27270648     


The p38 signaling pathway is activated upon AZD1208 treatment. OCI-M1 and OCI-M2 cells were treated with 2 μM AZD1208 for 4, 24, and 48 hours. Cell lysates were harvested and subjected to western blot analysis (n = 3). 

27270648
Immunofluorescence
p-Chk2; 

PubMed: 29879757     


Cells were treated with AZD1208 and AZD5363 alone or in combination for 5 days, and immunofluorescence analysis was subsequently performed. Confocal microscopy was used to observe the signals corresponding to p-Chk2 (red) and γ-H2AX (green). DAPI (blue) was used as a nuclear counterstain. CI, combination index. Scale bars=5 μm.

29879757
Growth inhibition assay
Cell viability; 

PubMed: 30654529     


93T449 and SW872 cells were treated with AZD1208 or vehicle control (DMSO; 0.1%) at the indicated concentrations and for the indicated times. The numbers of surviving cells were measured by cell count assay. The cell count assay was performed in triplicate. Data are means ± SE of three independent experiments. * p < 0.05 compared to the value of AZD1208 free control at the indicated time.

30654529
体内研究 AZD1208抑制与剂量成比例的MOLM-16和KG-1a异种移植肿瘤在体内的生长。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 75 mg/mL warmed (197.63 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 379.48
化学式

C21H21N3O2S

CAS号 1204144-28-4
储存条件 粉状
溶于溶剂
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    What is your recommended solvent of S7104 for mouse in vivo studies by oral administration?

  • 回答:

    1%CMC-Na is recommended and you will get a suspension. It is ok for oral administration.

  • 问题 2:

    I would like to ask which solvent I should use to dissolve AZD1208 for mouse study. Can AZD1208 be dissolved in 5% dextrose?

  • 回答:

    AZ1208 can be dissolved in 5% dextrose at 10 mg/ml as a suspension. If 5% Tween 80 added, the suspension will be more homogeneously.

Pim Signaling Pathway Map

相关Pim产品

Tags: 购买AZD1208 | AZD1208供应商 | 采购AZD1208 | AZD1208价格 | AZD1208生产 | 订购AZD1208 | AZD1208代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID