2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  3. JAK Syk
  4. Cerdulatinib

Cerdulatinib  (Synonyms: PRT062070; PRT2070)

目录号: HY-15999 纯度: 99.06%
COA 产品使用指南

摩尔计算器

Cerdulatinib (PRT062070) 是一种有效的选择性 Tyk2 抑制剂，IC50 为 0.5 nM。Cerdulatinib (PRT062070) 是 JAK 和 SYK 的双抑制剂，抑制JAK1，2，3 和SYK的 IC50 分别为12，6，8 和 32。

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Cerdulatinib Chemical Structure

Cerdulatinib Chemical Structure

CAS No. : 1198300-79-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥635
In-stock
1 mg ￥363
In-stock
5 mg ￥648
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10 mg ￥864
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25 mg ￥1475
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50 mg ￥2160
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100 mg ￥3300
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200 mg ￥4620
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500 mg 现货 询价
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Cerdulatinib:

Cerdulatinib 相关抗体

Top Publications Citing Use of Products

    Cerdulatinib purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367):eaan4368.  [Abstract]

    Immunoblot analysis in MV-4-11 cells and MOLM-13, FLT3-WT and FLT3-ITD transfected HEK293 cells, and Ba/F3 FLT3-ITD cells revealed FLT3 target engagement for Golvatinib and Cabozantinib.

    Cerdulatinib purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367):eaan4368.  [Abstract]

    Kinobead western Blot readout for selected inhibitor:protein combinations.

    查看 JAK 亚型特异性产品:

    查看所有亚型
    JAK1 JAK2 JAK3 Tyk2 JAK

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Cerdulatinib (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.

    IC50 & Target

    Tyk2

    0.5 nM (IC50)

    JAK2

    6 nM (IC50)

    JAK3

    8 nM (IC50)

    JAK1

    12 nM (IC50)

    Syk

    32 nM (IC50)

    MST1

    4 nM (IC50)

    ARK5

    4 nM (IC50)

    MLK1

    5 nM (IC50)

    FMS

    5 nM (IC50)

    AMPK

    6 nM (IC50)

    TBK1

    10 nM (IC50)

    MARK1

    10 nM (IC50)

    PAR1B-a

    13 nM (IC50)

    TSSK

    14 nM (IC50)

    MST2

    15 nM (IC50)

    GCK

    18 nM (IC50)

    JNK3

    18 nM (IC50)

    Rsk2

    20 nM (IC50)

    Rsk4

    28 nM (IC50)

    CHK1

    42 nM (IC50)

    Flt4

    51 nM (IC50)

    Flt3

    90 nM (IC50)

    Ret

    105 nM (IC50)

    Itk

    194 nM (IC50)

    体外研究
    (In Vitro)

    Cerdulatinib shows inhibitory effect on 60 CLL with IC50 ranging from 0.37 to 10.02 µM. Cerdulatinib induces apoptosis in CLL in association with MCL-1 down-regulation and PARP cleavage. Cerdulatinib (2μM) is able to overcome the support of the microenvironment and induces CLL cell death. Cerdulatinib (250-500 nM) blocks proliferation of ibrutinib-sensitive and ibrutinib-resistant primary CLL cells. Cerdulatinib also blocks proliferation of both ibrutinib-sensitive and ibrutinib-resistant primary CLL cells as well as BTKC481S-transfected cell lines, and blocks BCR and JAK-STAT signaling pathways. Furthermore, inhibition of SYK and JAK by cerdulatinib translates to downstream inhibition of AKT and ERK. Cerdulatinib inhibits the activity of NF-kB pathway[1]. PRT062070 reduces the ability of stimulated B cells to upregulate cell-surface expression of the early activation marker CD69 (IC50=0.11 µM). PRT062070 exhibits differential potency against cytokine JAK/STAT signaling pathways. PRT062070 (1 or 3 µM) induces apoptosis in BCR-signaling competent NHL cell lines[2]. Cerdulatinib demonstrates inhibitory activity against both ABC and GCB subtypes of DLBCL cells. Cerdulatinib also induces apoptosis in both GCB and ABC subtypes of DLBCL cell lines via caspase 3 and PARP cleavage. And cerdulatinib blocks cell cycle in both ABC and GCB subtypes of DLBCL via inhibition of RB phosphorylation and down-regulation of cyclin E. Cerdulatinib induces cell cycle arrest and apoptosis under the condition of BCR stimulation in all DLBCL cell lines. Besides, cerdulatinib blocks JAK/STAT and BCR signaling in both ABC and GCB DLBCL cell lines. Cerdulatinib induces cell death in primary human DLBCL samples[3]. Cerdulatinib inhibits BCR-induced signals in a dose-dependent manner and most strongly between 0.3 to 1 μM. and particularly in IGHV-unmutated samples with greater BCR signaling capacity and response to IL4, or samples expressing higher levels of sIgM, CD49d+, or ZAP70+. Cerdulatinib overcomes anti-IgM, IL4/CD40L, or NLC-mediated protection by preventing upregulation of MCL-1 and BCL-XL; however, BCL-2 expression is unaffected. Furthermore, in samples treated with IL4/CD40L, cerdulatinib synergizes with venetoclax in vitro to induce greater apoptosis than either drug alone[4].

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

    Cerdulatinib 相关抗体:
    体内研究
    (In Vivo)

    PRT062070 (0.5 mg/kg) results in a nonstatistically significant trend toward reduced ankle inflammation, whereas significant reductions in inflammation are achieved with the 1.5, 3, and 5 mg/kg doses. PRT062070 also affects anticollagen antibody formation. PRT062070 (15 mg/kg) suppresses upregulation of splenic B-cell surface CD80/86 and CD69, and inhibits BCR signaling and activation in the spleen after oral dosing in mice[2].

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

    445.54

    Formula

    C20H27N7O3S
    CAS 号
    性状

    固体

    颜色

    Light gray to khaki

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 30 mg/mL (67.33 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 2.2445 mL 11.2223 mL 22.4447 mL
    5 mM 0.4489 mL 2.2445 mL 4.4889 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 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

    动物实验：

    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: ≥ 2.5 mg/mL (5.61 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 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。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.61 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

    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

    只
    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）。
    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: 99.06%

    COA (284 KB) RP-HPLC (270 KB) LCMS (87 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    TMD8 cells are transfected with constructs of WT BTK or BTKC481S mutants using kit V, Program U-13 on Amaxa Nucleofector. After transfection, the cells are co-cultured with NKTert cells in a 24-well plate for 24 hrs for recovery. Ibrutinib, cerdulatinib and vehicle (DMSO) are then added into the transfected TMD8 cells and cellular viability is determined with MuseTM Count & Viability kit using Muse Cell Analyzer. The cell survival is determined by flow cytometry using the Annexin V/7-AAD Apoptosis Detection Kit I on freshly isolated CLL cells.

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

    Cerdulatinib 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2445 mL 11.2223 mL 22.4447 mL 56.1117 mL
    5 mM 0.4489 mL 2.2445 mL 4.4889 mL 11.2223 mL
    10 mM 0.2244 mL 1.1222 mL 2.2445 mL 5.6112 mL
    15 mM 0.1496 mL 0.7482 mL 1.4963 mL 3.7408 mL
    20 mM 0.1122 mL 0.5611 mL 1.1222 mL 2.8056 mL
    25 mM 0.0898 mL 0.4489 mL 0.8978 mL 2.2445 mL
    30 mM 0.0748 mL 0.3741 mL 0.7482 mL 1.8704 mL
    40 mM 0.0561 mL 0.2806 mL 0.5611 mL 1.4028 mL
    50 mM 0.0449 mL 0.2244 mL 0.4489 mL 1.1222 mL
    60 mM 0.0374 mL 0.1870 mL 0.3741 mL 0.9352 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.

    Keywords:

    Cerdulatinib1198300-79-6PRT062070 PRT2070PRT 062070PRT-062070PRT2070PRT 2070PRT-2070JAKSykJanus kinaseSpleen tyrosine kinaseInhibitorinhibitorinhibit

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