GDC-0152

For research use only. Not for use in humans.

目录号:S7010

GDC-0152 Chemical Structure

Molecular Weight(MW): 498.64

GDC-0152是一种有效的XIAP-BIR3,ML-IAP-BIR3,cIAP1-BIR3和cIAP2-BIR3拮抗剂,无细胞试验中Ki分别为28 nM,14 nM,17 nM和43 nM,对cIAP1-BIR2和cIAP2-BIR2具较低亲和力。Phase 1。

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RMB 2225.28 现货
RMB 13677.3 现货
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客户使用Selleck生产的GDC-0152发表文献13篇:

客户使用该产品的3个实验数据:

  • Inhibitor of Apoptosis Proteins (IAPs) were involved in MCP-1/IL-6 production under high dose TNF-α stimulation. A. hUC-MSCs (2x104 in 96-well plates) were pretreated for 2h with the IAP inhibitor GDC-0152 at increasing concentrations (0-1000 nM), then stimulated with TNF-α (20 ng/ml, 1.2 nM). After a further 24h, trypan blue was used to exclude cell toxicity. SN was collected and IL-6 and MCP-1 concentrations were measured by ELISA. B. hUC-MSCs(5×105 in T25 bottle) were pretreated with GDC-0152(1000nM) for 2 h, then stimulated with TNF-α (20 ng/ml, 1.2 nM). 24 hours later, protein from nucleus and cytoplasma were extracted separately and the amount of NF-kB were detected by Western blot. Data are as mean±SEM of triplicate measurements; *p<0.05, **p<0.01, ***p<0.001 when compared to untreated cells. These experiments were repeated 3 times with the same results, using clone 69 and another TNF-α sensitive clone (clone 120003).

    PLoS One, 2015, 10(5):e0128647.. GDC-0152 purchased from Selleck.

  • (a) Apoptosis (SubG0/G1) of DMSO control and GDC-0152-treated cells was determined by flow cytometry of propidium iodide-stained nuclei and percentage of apoptosis is shown. U87MG and GL261 cell lines were treated for 72 h and GBM6 and GBM9 cell lines were treated for 8 days at the indicated concentrations. At these respective time points, percentage of U87MG cells dead by apoptosis, percentage of GL261 cells, percentage of GBM6 cells and percentage of GBM9 cells. Data are expressed as mean+S.E.M. Three independent experiments were performed for the GL261 cell lines and five for the U87MG, GBM6 and GBM9 cell lines. *P<0.05; **P<0.01; ***P<0.005.

    Cell Death Dis, 2016, 7(8):e2325. GDC-0152 purchased from Selleck.

  • GDC-0152 sensitises FTC cell lines for TRAIL-induced apoptosis. FTC cell lines were treated with increasing concentrations of rh-TRAIL with and without Smac mimetics GDC-0152. Changes in cell viability are illustrated linearly in percentage control and stratified according to the FP. While FTC cell line TT2609-bib2 was susceptible to rh-TRAIL alone (C), cell line FTC133 proved to be resistant to rh-TRAIL-induced apoptosis (D). Smac mimetic treatment alone had no impact on cell viability. Annexin V/PI staining and FACS analyses of FTC cells demonstrate the changes of annexin positive apoptotic cells after incubation with rh-TRAIL alone (−) or in combination (+) with Smac mimetics Birinapant GDC-0152 (C/D). Changes in protein expression of cIAP1/2 after treatment with the respective Smac mimetic are illustrated using Western blot. GAPDH served as loading control. Blots are cropped to increase clarity. Statistical significance was calculated by two-tailed nonparametric Mann–Whitney test. e. survival:expected survival; sp. survival: specific survival; FP: fractional product; *P < 0.05; **P < 0.01.

    Endocr Relat Cancer, 2018, 25(3):295-308. GDC-0152 purchased from Selleck.

产品安全说明书

IAP抑制剂选择性比较

生物活性

产品描述 GDC-0152是一种有效的XIAP-BIR3,ML-IAP-BIR3,cIAP1-BIR3和cIAP2-BIR3拮抗剂,无细胞试验中Ki分别为28 nM,14 nM,17 nM和43 nM,对cIAP1-BIR2和cIAP2-BIR2具较低亲和力。Phase 1。
靶点
MLXBIR3SG [1]
(Cell-free assay)
cIAP1-BIR3 [1]
(Cell-free assay)
XIAP-BIR3 [1]
(Cell-free assay)
cIAP2-BIR3 [1]
(Cell-free assay)
XIAP-BIR2 [1]
(Cell-free assay)
14 nM(Ki) 17 nM(Ki) 28 nM(Ki) 43 nM(Ki) 112 nM(Ki)
体外研究

GDC-0152可阻断IAP蛋白和促凋亡分子参与的蛋白质-蛋白质的相互作用。GDC-0152瞬时转染HEK293T细胞,表现为扰乱XIAP结合部分处理的caspase-9并扰乱ML-IAP,CIAP1,cIAP2和Smac蛋白的结合。在黑色素瘤SK-MEL28细胞中,GDC-0152有效抑制ML-IAP和Smac蛋白的内源性结合。在MDA-MB-231乳腺癌细胞系中,GDC-0152导致细胞活力下降,而对正常的人乳腺上皮细胞(HMEC)没有影响。GDC-0152以剂量和时间依赖性方式激活胱天蛋白酶3和7。在A2058黑色素瘤细胞中,GDC-0152诱导CIAP1的快速降解。在浓度低至10 nM时,它有效地诱导了CIAP1降解,这和其对CIAP1亲和力一致。

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293T cells NFXm[oZHfW6ldHnvckBie3OjeR?= M37OOFEuPTBizszN Mlm4NkBp NWjqSlU{UW6qaXLpeIlwdiCxZjDGcIFoNXSjZ3fl[EBZUUGSIFLJVlMh\G:vYXnuJIJqdmSrbnegeI8h[0mDUEGg[ZhxemW|c3XkJIlvKGi3bXHuJGhGUzJ7M2SgZ4VtdHNiYYSgNUB1dyB3MDD1UUBi\nSncjCyJIhzeyCkeTDpcY12dm:ycnXjbZBqfGG2aX;u MkDLNlI1OTN6NkO=
SK-MEL28 cells NGm0ZlZHfW6ldHnvckBie3OjeR?= M3LmW|AvPSEQvF2= MVnJcohq[mm2aX;uJI9nKE2OLVnBVEBjcW6maX7nJJRwKFOvYYig[ZhxemW|c3XkJIlvKGenbXPpeIFjcW6nIHHu[EB7XkGmIITy[YF1\WRiaIXtZY4hW0tvTVXMNlgh[2WubIOgZZQhOC53IIXNJIJ6KGmvbYXuc5Bz\WOrcHn0ZZRqd25? NH7HWIczOjRzM{i2Ny=>
A2058 cells NE\jR|BHfW6ldHnvckBie3OjeR?= MYWxOUBucW6| M3fF[mlv\HWldHnvckBw\iCycn;0[YF{d22jbDDk[Ydz[WSjdHnvckBw\iClSVHQNUBqdiCqdX3hckBCOjB3ODDj[YxteyCjZoTldkAyPSCvaX7zJIJ6KGmvbYXuc4Jtd3S2aX7n MYKyNlQyOzh4Mx?=
MDA-MB-231 cells NXew[5N[S3m2b4TvfIlkcXS7IHHzd4F6 MkTGO|IhcA>? NVO4WIhSS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW|Y3XueEBie3OjeR?= MoXGNlI1OTN6NkO=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
cIAP1 / cIAP2 / XIAP / ML-IAP ; 

PubMed: 27490930     


Expression levels of cIAP1, cIAP2, XIAP and ML-IAP were analyzed by western blotting. Cell lines were treated with 1 μM of GDC-0152. U87MG and GL261 were treated for 72 h and GBM6 and GBM9 cell lines for 8 days. In all GBM cell lines GDC-0152 decreased IAP expression. Expression level of β-actin served as loading control. A representative experiment of three experiments is shown

27490930
体内研究 GDC-0152具有基于使用人肝微粒体进行代谢稳定性分析的预测的中度肝清除作用。血浆蛋白和GDC-0152的结合是中度的,在(0.1−100 μM)浓度时,结合率在小鼠(88-91%),大鼠(89-91%),狗(81-90%),猴(76-85%)和人类(75 - 83%)中没有差别;而在兔(95-96%)中较高。在测试的所有物种中血液血浆分配比范围从0.6到1.1,GDC-0152并不优先分布在红血细胞中。 GDC-0152的药代动力学是Cmax为53.7 μM,AUC为203.5 h•μM。[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)

激酶实验:[1]
- 合并

荧光偏振为基础的竞争分析:

拮抗剂的抑制常数(Ki)通过如下方法测定:将IAP蛋白构建添加到含有不同稀释倍数的拮抗剂或AVPW肽中,将HID-FAM探针或AVP-diPhe-FAM探针添加到偏振缓冲中。样品在孵育30分钟后读数。荧光偏振值是拮抗剂浓度的函数,并且IC 50值是通过使用软件将数据拟合到4-参数方程获得。Ki的拮抗剂值由IC50值确定。
细胞实验:[1]
- 合并
  • Cell lines: MDA-MB-231, 正常人乳腺上皮细胞(人微血管内皮细胞)
  • Concentrations: ~1 μM
  • Incubation Time: 72 小时
  • Method: MDA-MB-231乳腺癌细胞和人微血管内皮细胞用指定浓度的GDC-0152处理。细胞死亡是使用的CellTiter-Glo发光细胞存活力测定在处理72小时后检测。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: MDA-MB-231乳腺癌异种移植小鼠模型
  • Dosages: 10, 50或100 毫克/千克
  • Administration: 口服灌胃
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 99 mg/mL (198.54 mM)
Ethanol 99 mg/mL (198.54 mM)
Water 3 mg/mL (6.01 mM)
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
30% propylene glycol, 5% Tween 80, 65% D5W
5 mg/mL

* 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 498.64
化学式

C25H34N6O3S

CAS号 873652-48-3
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

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

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操作手册

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IAP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID