1. Cell Cycle/DNA Damage Apoptosis
  2. CDK Apoptosis
  3. Asnuciclib

Asnuciclib  (Synonyms: CDKI-73; LS-007)

目录号: HY-12445 纯度: 98.63%
COA 产品使用指南

Asnuciclib (CDKI-73; LS-007) 是具有口服活性的、高效的 CDK9 抑制剂,其对CDK9、CDK1 和 CDK2Ki 值分别为 4 nM、4 nM 和 3 nM。CDKI-73 可下调 RNA 聚合酶 II 的磷酸化。Asnuciclib 也是一种 Rab11 的抑制剂。

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Asnuciclib Chemical Structure

Asnuciclib Chemical Structure

CAS No. : 1421693-22-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3850
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1 mg ¥1600
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2 mg ¥2333
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5 mg ¥3500
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10 mg ¥5000
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Top Publications Citing Use of Products

    Asnuciclib purchased from MCE. Usage Cited in: Am J Cancer Res. 2020 Apr 1;10(4):1140-1155.   [Abstract]

    The expression of BRCA1, p-CDK9, CDK9, Bcl-2 proteins, γ-H2AX, cleaved PARP, and cleaved caspase-3 in HO8910 cells treated with CDKI-73.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Asnuciclib (CDKI-73; LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. Asnuciclib down-regulates the RNAPII phosphorylation. Asnuciclib is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion[1][2][3][4].

    IC50 & Target[6][1]

    CDK2

    3.27 nM (IC50)

    CDK9

    5.78 nM (IC50)

    CDK1

    8.17 nM (IC50)

    CDK4

    8.18 nM (IC50)

    CDK6

    37.68 nM (IC50)

    CDK7

    134.26 nM (IC50)

    CDK1

    4 nM (Ki)

    CDK2

    3 nM (Ki)

    CDK9

    4 nM (Ki)

    CDK7

    91 nM (Ki)

    体外研究
    (In Vitro)

    Asnuciclib is highly cytotoxic to primary leukemia cells derived from CLL patients (mean LD50 = 0.08 μM) and shows>500-fold selectivity for primary leukemia cells over normal B-lymphocytes (LD50=40.5 μM)[1].
    Asnuciclib (0.1 μM, 4 h) inhibits the phosphorylation of serine 2 of RNA polymerase II and MCL1 protein expression in CLL cells[1].
    Asnuciclib induced caspase-dependent apoptosis that was preceded by dephosphorylation of cdk9 and serine 2 of RNA polymerase II[1].
    Asnuciclib is highly effective against all cell lines tested with an IC50 in the range of 0.012-0.517 μM; in particular three MLL-AML cell lines, namely MOLM13, MV4-11 and THP-1, were highly sensitive to CDKI-73 with IC50 values <0.062 μM[3].

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

    Cell Viability Assay[1].

    Cell Line: CLL cells.
    Concentration: 0-1 μM.
    Incubation Time: 48 h.
    Result: Shows preferential cytotoxicity in CLL cells.
    体内研究
    (In Vivo)

    Asnuciclib (25, 50, 100 mg/kg) markedly decreases tumor growth in a dose-dependent manner and results in a prolongation of animal life span (P < 0.001) without causing body weight loss and other overt toxicities.[3].

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

    Animal Model: MV4-11 tumor bearing mice[3].
    Dosage: 25 mg/kg.
    Administration: Orally once everyday for 33 days.
    Result: Caused a remarkable delay in tumor growth compared to vehicle-treated mice, as reflected in a percentage for the mean tumor volume in treated to control mice of 43% at day 31.
    Animal Model: Balb/C mice aged 6-8 weeks[3].
    Dosage: 2 mg/kg (IV), 10, 20 and 40 mg/kg (PO). (Pharmacokinetic Analysis.)
    Administration: IV and PO, single dose.
    Result: The Cmax increased from 1.29 to 3.66 μM at a mean time of 1 h and the area under the curve (AUC) of CDKI-73 increased from 3.51 to 12.8 μM.h when the oral dose was escalated from 10 to 40 mg/kg.
    CDKI-73 was eliminated from plasma with a mean terminal half-life (T1/2) of 2 h. Its oral bioavailability (F) ranged from 54 to 85% across the three doses.
    分子量

    394.45

    Formula

    C15H15FN6O2S2

    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 52 mg/mL (131.83 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 2.5352 mL 12.6759 mL 25.3518 mL
    5 mM 0.5070 mL 2.5352 mL 5.0704 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 (stored under nitrogen)。-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。

    • 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

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    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: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.67 mg/mL (6.77 mM); 澄清溶液

      此方案可获得 ≥ 2.67 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 26.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    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
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.76%

    参考文献

    Asnuciclib 相关分类

    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 (stored under nitrogen)。-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 1 mM 2.5352 mL 12.6759 mL 25.3518 mL 63.3794 mL
    5 mM 0.5070 mL 2.5352 mL 5.0704 mL 12.6759 mL
    10 mM 0.2535 mL 1.2676 mL 2.5352 mL 6.3379 mL
    15 mM 0.1690 mL 0.8451 mL 1.6901 mL 4.2253 mL
    20 mM 0.1268 mL 0.6338 mL 1.2676 mL 3.1690 mL
    25 mM 0.1014 mL 0.5070 mL 1.0141 mL 2.5352 mL
    30 mM 0.0845 mL 0.4225 mL 0.8451 mL 2.1126 mL
    40 mM 0.0634 mL 0.3169 mL 0.6338 mL 1.5845 mL
    50 mM 0.0507 mL 0.2535 mL 0.5070 mL 1.2676 mL
    60 mM 0.0423 mL 0.2113 mL 0.4225 mL 1.0563 mL
    80 mM 0.0317 mL 0.1584 mL 0.3169 mL 0.7922 mL
    100 mM 0.0254 mL 0.1268 mL 0.2535 mL 0.6338 mL
    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:
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