1. GPCR/G Protein Immunology/Inflammation Anti-infection
  2. CXCR HIV
  3. AMD 3465

AMD 3465  (Synonyms: GENZ-644494)

目录号: HY-15971A 纯度: 99.59%
COA 产品使用指南

AMD 3465 (GENZ-644494) 是一种有效的 CXCR4 拮抗剂,在 SupT1 细胞中,能够抑制 12G5 mAb,CXCL12AF647CXCR4 结合,IC50 值分别为 0.75 nM 和 18 nM;AMD 3465 同时可有效抑制 X4 HIV 的复制 (IC50,1-10 nM),但对 R5 HIV 病毒无作用。

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AMD 3465 Chemical Structure

AMD 3465 Chemical Structure

CAS No. : 185991-24-6

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5 mg ¥1860
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10 mg ¥2800
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100 mg   询价  

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Other Forms of AMD 3465:

    AMD 3465 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2021 Mar 24;138:111476.  [Abstract]

    The results of western blotting showed that high glucose inhibited the activation of the cell cycle pathway, the expression level of CDK4, CDK6, Nusap1, and Cyclin D1 are reduced. However, under the action of AMD3465 (10 μM), the expression level of proteins is significantly higher than that of the HG group.

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    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.

    IC50 & Target[1]

    12G5 mAb-CXCR4

    0.75 nM (IC50, in SupT1 cells)

    CXCL12AF647-CXCR4

    18 nM (IC50, in SupT1 cells)

    X4 HIV-1 (IIIB)

    12.3 nM (IC50, in MT-4 cells)

    X4 HIV-1 (NL4.3)

    6.1 nM (IC50, in MT-4 cells)

    X4 HIV-1 (NL4.3AMD3100)

    2822 nM (IC50, in MT-4 cells)

    X4 HIV-1 (RF)

    7.4 nM (IC50, in MT-4 cells)

    X4 HIV-1 (HE)

    9.8 nM (IC50, in MT-4 cells)

    HIV-2 (ROD)

    12.3 nM (IC50, in MT-4 cells)

    HIV-2 (EHO)

    12.3 nM (IC50, in MT-4 cells)

    体外研究
    (In Vitro)

    AMD 3465 is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells. AMD 3465 (50 nM) totally blocks CXCL12-induced calcium mobilization, with an IC50 of 17 nM, but shows no effect on the intracellular calcium fluxes elicited by the CCR5 ligands RANTES, LD78β and MIP-1β in U87.CD4.CCR5 cells. AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses. AMD3465 is cytotoxic to the X4 HIV-1 strains IIIB, NL4.3, RF and HE with an IC50 ranging from 6 to 12 nM. The IC50 for suppression of the HIV-2 strains ROD and EHO is 12.3 nM[1]. AMD 3465 inhibits CXCL-12-induced growth in U87 and Daoy cells. AMD 3465 treatment stimulates the phosphorylation of Erk1/2 in U87 and Daoy cells[2].

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

    体内研究
    (In Vivo)

    AMD 3465 (2.5 mg/kg/d, s.c. for 5 weeks) significantly blocks the growth of U87 GBM and Daoy xenografts[2].

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

    分子量

    410.60

    Formula

    C24H38N6

    CAS 号
    性状

    固液混合物

    颜色

    Off-white to light yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    -20°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶解性数据
    细胞实验: 

    H2O 中的溶解度 : ≥ 100 mg/mL (243.55 mM)

    * "≥" 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 2.4355 mL 12.1773 mL 24.3546 mL
    5 mM 0.4871 mL 2.4355 mL 4.8709 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 (protect from light)。-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

    纯度: 99.59%

    参考文献
    Cell Assay
    [2]

    Following serum starvation for 24 h, astrocytes, granule cells, U87 cells, and Daoy cells are treated with 1 μg/mL CXCL12, 2.5 ng/mL AMD 3465, 200 μM rolipram, or 10 μM forskolin. Daoy and U87 cell growth in culture is measured by trypan blue exclusion after 24 and 48 h of treatment, respectively[2].

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

    Animal Administration
    [2]

    Mice[2]
    Mice are imaged at least twice after implantation of cells to identify those with equivalent tumor growth rates. Two weeks after tumor cell implantation, cohorts of mice with approximately equivalent tumor bioluminescence are divided into equal control and treatment groups. Animals in AMD 3465 experiments receive s.c. osmotic pumps loaded with 10 mg/mL AMD 3465 in sterile PBS or PBS alone. The infusion rate is 0.25 μL/h (50 μg/d). For the experiments with rolipram or caffeine, mice in the treatment groups receive oral administration of rolipram (5 μg/g/d) or caffeine (100 μg/g/d). The concentration of drug in the water is determined from daily measurements of water consumption by each animal over the course of 7 days. Concentrations are adjusted based on water consumption to provide the prescribed dose[2].

    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 (protect from light)。-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
    H2O 1 mM 2.4355 mL 12.1773 mL 24.3546 mL 60.8865 mL
    5 mM 0.4871 mL 2.4355 mL 4.8709 mL 12.1773 mL
    10 mM 0.2435 mL 1.2177 mL 2.4355 mL 6.0887 mL
    15 mM 0.1624 mL 0.8118 mL 1.6236 mL 4.0591 mL
    20 mM 0.1218 mL 0.6089 mL 1.2177 mL 3.0443 mL
    25 mM 0.0974 mL 0.4871 mL 0.9742 mL 2.4355 mL
    30 mM 0.0812 mL 0.4059 mL 0.8118 mL 2.0296 mL
    40 mM 0.0609 mL 0.3044 mL 0.6089 mL 1.5222 mL
    50 mM 0.0487 mL 0.2435 mL 0.4871 mL 1.2177 mL
    60 mM 0.0406 mL 0.2030 mL 0.4059 mL 1.0148 mL
    80 mM 0.0304 mL 0.1522 mL 0.3044 mL 0.7611 mL
    100 mM 0.0244 mL 0.1218 mL 0.2435 mL 0.6089 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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    产品名称:
    AMD 3465
    目录号:
    HY-15971A
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