1. Cell Cycle/DNA Damage Epigenetics Autophagy
  2. PARP Autophagy
  3. Veliparib dihydrochloride

Veliparib dihydrochloride  (Synonyms: 维利帕尼二盐酸盐; ABT-888 dihydrochloride)

目录号: HY-10130 纯度: 99.96%
COA 产品使用指南

Veliparib dihydrochloride是有效的 PARP1PARP2 抑制剂,Ki 分别为5.2 nM,2.9 nM。

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Veliparib dihydrochloride Chemical Structure

Veliparib dihydrochloride Chemical Structure

CAS No. : 912445-05-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥462
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5 mg ¥420
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10 mg ¥680
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50 mg ¥1800
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100 mg ¥3000
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200 mg ¥4500
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1 g   询价  

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Customer Review

Other Forms of Veliparib dihydrochloride:

MCE 顾客使用本产品发表的 31 篇科研文献

Proliferation Assay
WB

    Veliparib dihydrochloride purchased from MCE. Usage Cited in: J Vet Med Sci. 2018 Nov 23;80(11):1775-1781.  [Abstract]

    PK-15 cells are incubated with 20 μM ABT-888 for 1 hr and subsequently infected with transmissible gastroenteritis virus (TGEV) for 36 hr. Cells are collected and then subjected to Western blot analysis for PARP-1.

    Veliparib dihydrochloride purchased from MCE. Usage Cited in: Electrostatics Joint Conference. 2016 July.

    Dose curve of Veliparib on MDA-MB-231 cells without Electroporation.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively.

    IC50 & Target[1]

    PARP-2

    2.9 nM (Ki)

    PARP-1

    5.2 nM (Ki)

    体外研究
    (In Vitro)

    Veliparib 对 SIRT2 (>5 μM)没有活性。[1]
    Veliparib 抑制 C41 细胞中的 PARP 活性,EC50 为 2 nM[2]。Veliparib 可以降低受照射和未受照射的 H460 细胞中的 PAR 水平。Veliparib 通过抑制 H460 细胞中的 PARP-1 降低克隆形成存活并抑制 DNA 修复。与放疗联合使用时,Veliparib 可增加 H460 细胞的凋亡和自噬[3]。Veliparib 抑制 H1299、DU145 和 22RV1 细胞中的 PARP 活性,并且抑制与 p53 功能无关。Veliparib (10 μM) 在克隆形成的 H1299 细胞中将存活分数 (SF) 抑制 43%。Veliparib 在含氧 H1299 细胞中表现出有效的放射敏感性。Veliparib 可以减弱 H1299、DU145 和 22RV1[4]等低氧照射细胞的 SF。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Veliparib在小鼠、SD大鼠、比格犬和食蟹猴口服给药后的口服生物利用度为 56%-92%[1]。Veliparib (25 mg/kg,ip) 可以改善 NCI-H460 异种移植模型中的肿瘤生长延迟。结合放疗,veliparib 可减少肿瘤血管形成[3]。在 A375 和 Colo829 异种移植模型中,Veliparib 以 3 和 12.5 mg/kg 的剂量将肿瘤内 PAR 水平降低 95% 以上,并且这种抑制可以随着时间的推移而维持[4]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    317.21

    Formula

    C13H18Cl2N4O

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    维利帕尼二盐酸盐

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    细胞实验: 

    H2O 中的溶解度 : 250 mg/mL (788.12 mM; 超声助溶)

    DMSO 中的溶解度 : ≥ 3.2 mg/mL (10.09 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.1525 mL 15.7624 mL 31.5249 mL
    5 mM 0.6305 mL 3.1525 mL 6.3050 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: PBS

      Solubility: 100 mg/mL (315.25 mM); 澄清溶液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
    纯度 & 产品资料
    参考文献
    Kinase Assay
    [1]

    PARP assays are conducted in a buffer containing 50 mM Tris (pH 8.0), 1 mM DTT, 1.5 μM [3H]NAD+ (1.6 μCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Reactions are terminated with 1.5 mM benzamide, transferred to streptavidin Flash plates, and counted using a TopCount microplate scintillation counter.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    For B16F10 syngeneic studies, 6×104 cells are mixed with 50% Matrigel and inoculated by s.c. injection into the flank of 6- to 8-week-old female C57BL/6 mice (20 g). For cisplatin efficacy studies, female nude mice are implanted s.c. by trocar with fragments (20-30 mm3) of human tumors harvested from s.c. grown tumors in nude mice hosts. For the carboplatin and MX-1 cyclophosphamide studies, female scid mice are inoculated with 200 μL of a 1:10 dilution of tumor brei in 45% Matrigel and 45% Spinner MEM. For these established tumor studies, tumors are allowed to grow to the indicated size and then randomized to therapy groups. For DOHH-2 xenograft studies, 1×106 cells are mixed with 50% Matrigel and inoculated by s.c. injection into the flank of male scid mice. Veliparib is delivered by either oral route or continuous infusion using s.c. placement of 14-day Alzet OMP model 2002 in a vehicle containing 0.9% NaCl adjusted to pH 4.0. The OMP delivers at a rate of 12 μL daily and Veliparib doses are calculated accordingly. Temozolomide, cisplatin, carboplatin, and cyclophosphamide are formulated according to the manufacturers' recommendations.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 3.1525 mL 15.7624 mL 31.5249 mL 78.8121 mL
    5 mM 0.6305 mL 3.1525 mL 6.3050 mL 15.7624 mL
    10 mM 0.3152 mL 1.5762 mL 3.1525 mL 7.8812 mL
    H2O 15 mM 0.2102 mL 1.0508 mL 2.1017 mL 5.2541 mL
    20 mM 0.1576 mL 0.7881 mL 1.5762 mL 3.9406 mL
    25 mM 0.1261 mL 0.6305 mL 1.2610 mL 3.1525 mL
    30 mM 0.1051 mL 0.5254 mL 1.0508 mL 2.6271 mL
    40 mM 0.0788 mL 0.3941 mL 0.7881 mL 1.9703 mL
    50 mM 0.0630 mL 0.3152 mL 0.6305 mL 1.5762 mL
    60 mM 0.0525 mL 0.2627 mL 0.5254 mL 1.3135 mL
    80 mM 0.0394 mL 0.1970 mL 0.3941 mL 0.9852 mL
    100 mM 0.0315 mL 0.1576 mL 0.3152 mL 0.7881 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    目录号:
    HY-10130
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