1. PI3K/Akt/mTOR Epigenetics Cell Cycle/DNA Damage Apoptosis
  2. PI3K HDAC Apoptosis
  3. Fimepinostat

Fimepinostat  (Synonyms: CUDC-907)

目录号: HY-13522 纯度: 99.95%
COA 产品使用指南

Fimepinostat (CUDC-907) 有效抑制 I 型 PI3K 及 I 和 II 型 HDAC 酶,作用于 PI3Kα/PI3Kβ/PI3Kδ 和 HDAC1/HDAC2/HDAC3/HDAC10 ,IC50 分别为 19/54/39 nM 和 1.7/5.0/1.8/2.8 nM。

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Fimepinostat Chemical Structure

Fimepinostat Chemical Structure

CAS No. : 1339928-25-4

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Customer Review

Other Forms of Fimepinostat:

    Fimepinostat purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):677-688  [Abstract]

    Aspc-1 and Capan-1 cells are collected for Western blotting with the indicated antibodies after treatment with CUDC-907 for 48 h.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.

    IC50 & Target[1]

    PI3Kα

    19 nM (IC50)

    PI3Kδ

    39 nM (IC50)

    PI3Kβ

    54 nM (IC50)

    PI3Kγ

    311 nM (IC50)

    HDAC1

    1.7 nM (IC50)

    HDAC3

    1.8 nM (IC50)

    HDAC10

    2.8 nM (IC50)

    HDAC2

    5 nM (IC50)

    HDAC11

    5.4 nM (IC50)

    HDAC6

    27 nM (IC50)

    HDAC8

    191 nM (IC50)

    HDAC4

    409 nM (IC50)

    HDAC7

    426 nM (IC50)

    HDAC9

    554 nM (IC50)

    HDAC5

    674 nM (IC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A2780 EC50
    126.25 nM
    Compound: CUDC-907
    Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay
    Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay
    [PMID: 27186676]
    A2780 EC50
    221.75 nM
    Compound: CUDC-907
    Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay
    Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay
    [PMID: 27186676]
    A2780 IC50
    6.15 nM
    Compound: CUDC-907
    Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay
    Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay
    [PMID: 27186676]
    Bel-7402 IC50
    0.013 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay
    Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    Capan-2 IC50
    0.007 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay
    Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    DU-145 IC50
    0.56 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay
    Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    HCT-116 IC50
    0.005 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    HCT-116 IC50
    7.34 nM
    Compound: CUDC-907
    Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay
    Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay
    [PMID: 27186676]
    HCT-8 IC50
    0.005 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay
    Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    HeLa IC50
    6.8 nM
    Compound: CUDC-907
    Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Leu-Gly-Lys (Ac)-AMC as substrate after 30 mins by fluorescence assay
    Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Leu-Gly-Lys (Ac)-AMC as substrate after 30 mins by fluorescence assay
    [PMID: 27186676]
    HepG2 IC50
    0.015 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    HGC-27 IC50
    0.041 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay
    Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    Huh-7 IC50
    0.56 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay
    Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    K562 IC50
    0.28 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human K562 cells after 96 hrs by MTT assay
    Antiproliferative activity against human K562 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    MCF7 IC50
    0.041 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    MDA-MB-453 IC50
    0.009 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    MV4-11 IC50
    0.43 nM
    Compound: CUDC-907
    Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay
    Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay
    [PMID: 27186676]
    NCI-H1299 IC50
    0.025 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay
    Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    NCI-H460 IC50
    0.15 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay
    Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    Sf9 IC50
    0.36 nM
    Compound: 10; CUDC-907
    Inhibition of recombinant C-terminal His/FLAG-tagged HDAC1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
    Inhibition of recombinant C-terminal His/FLAG-tagged HDAC1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
    [PMID: 31117517]
    Sf9 IC50
    1.4 nM
    Compound: 10; CUDC-907
    Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
    Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
    [PMID: 31117517]
    Sf9 IC50
    1.6 nM
    Compound: 10; CUDC-907
    Inhibition of recombinant human full length HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
    Inhibition of recombinant human full length HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
    [PMID: 31117517]
    Sf9 IC50
    1.8 nM
    Compound: CUDC-907
    Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substr
    Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substr
    [PMID: 27186676]
    Sf9 IC50
    132 nM
    Compound: 10; CUDC-907
    Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
    Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
    [PMID: 31117517]
    Sf9 IC50
    19 nM
    Compound: CUDC-907
    Inhibition of full length recombinant human N-terminal GST-tagged p110 alpha/untagged p85 alpha expressed in baculovirus infected insect Sf9 cells using PI:3PS as substrate incubated for 60 mins by ADP-Glo luminescence assay
    Inhibition of full length recombinant human N-terminal GST-tagged p110 alpha/untagged p85 alpha expressed in baculovirus infected insect Sf9 cells using PI:3PS as substrate incubated for 60 mins by ADP-Glo luminescence assay
    [PMID: 27186676]
    Sf9 IC50
    19 nM
    Compound: 24; CUDC-907
    Inhibition of recombinant human full-length N-terminal GST-tagged p110alpha/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay
    Inhibition of recombinant human full-length N-terminal GST-tagged p110alpha/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay
    [PMID: 30418766]
    Sf9 IC50
    191 nM
    Compound: CUDC-907
    Inhibition of full length C-terminal His-tagged human recombinant HDAC8 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after
    Inhibition of full length C-terminal His-tagged human recombinant HDAC8 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after
    [PMID: 27186676]
    Sf9 IC50
    2.8 nM
    Compound: CUDC-907
    Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay
    Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay
    [PMID: 27186676]
    Sf9 IC50
    27 nM
    Compound: CUDC-907
    Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a
    Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a
    [PMID: 27186676]
    Sf9 IC50
    39 nM
    Compound: CUDC-907
    Inhibition of N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected insect Sf9 cells incubated for 2 hrs by kinase-glo assay
    Inhibition of N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected insect Sf9 cells incubated for 2 hrs by kinase-glo assay
    [PMID: 27186676]
    Sf9 IC50
    39 nM
    Compound: 24; CUDC-907
    Inhibition of recombinant human full-length N-terminal GST-tagged p110delta/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay
    Inhibition of recombinant human full-length N-terminal GST-tagged p110delta/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay
    [PMID: 30418766]
    Sf9 IC50
    409 nM
    Compound: CUDC-907
    Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrat
    Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrat
    [PMID: 27186676]
    Sf9 IC50
    426 nM
    Compound: CUDC-907
    Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measu
    Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measu
    [PMID: 27186676]
    Sf9 IC50
    445 nM
    Compound: 10; CUDC-907
    Inhibition of recombinant human full length HDAC4 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
    Inhibition of recombinant human full length HDAC4 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
    [PMID: 31117517]
    Sf9 IC50
    5 nM
    Compound: CUDC-907
    Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a
    Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a
    [PMID: 27186676]
    Sf9 IC50
    5.4 nM
    Compound: CUDC-907
    Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence
    Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence
    [PMID: 27186676]
    Sf9 IC50
    54 nM
    Compound: CUDC-907
    Inhibition of recombinant human p110beta expressed in baculovirus infected insect Sf9 cells incubated for 1 hr by ADP-gloreagen assay
    Inhibition of recombinant human p110beta expressed in baculovirus infected insect Sf9 cells incubated for 1 hr by ADP-gloreagen assay
    [PMID: 27186676]
    Sf9 IC50
    54 nM
    Compound: 24; CUDC-907
    Inhibition of recombinant human full-length N-terminal GST-tagged p110beta/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay
    Inhibition of recombinant human full-length N-terminal GST-tagged p110beta/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay
    [PMID: 30418766]
    Sf9 IC50
    554 nM
    Compound: CUDC-907
    Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition meas
    Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition meas
    [PMID: 27186676]
    Sf9 IC50
    674 nM
    Compound: CUDC-907
    Inhibition of human recombinant HDAC5 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay
    Inhibition of human recombinant HDAC5 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay
    [PMID: 27186676]
    SW1990 IC50
    0.18 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay
    Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    U-87MG ATCC IC50
    0.007 μM
    Compound: 10; CUDC-907
    Antiproliferative activity against human U87 cells after 96 hrs by MTT assay
    Antiproliferative activity against human U87 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    体外研究
    (In Vitro)

    Fimepinostat 是一种有效的 HDAC I 类和 II 类酶泛抑制剂,观察到它对 I 类 HDAC 的效力与 LBH589 相似,但高于 SAHA。Fimepinostat 也是 I 类 PI3K 激酶的有效抑制剂,对 PI3Kα、PI3Kβ 和 PI3Kδ 的 IC50 分别为 19、54 和 39 nM。Fimepinostat 显著诱导 H460 中的 p21 蛋白,H460 是一种非小细胞肺癌 (NSCLC) 细胞系。Fimepinostat 导致 RPMI-8226 多发性骨髓瘤细胞中 p-STAT3 (Y-705) 和 p-SRC 的减少,并降低 H1975 NSCLC 细胞和 BT-分别为 474 个乳腺癌细胞。Fimepinostat 以剂量依赖性方式诱导 HCT-116 结肠癌细胞中的 caspase-3 和-7 激活。Fimepinostat 有效抑制源自血液肿瘤和实体瘤的癌细胞的生长。Fimepinostat 有效抑制表达突变型或野生型 PI3K 的细胞的增殖[1]

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

    体内研究
    (In Vivo)

    口服 Fimepinostat 以剂量依赖性方式抑制 Daudi 癌细胞异种移植物的生长。在该模型中观察到 100 mg/kg 的肿瘤停滞而没有明显的毒性。重要的是,在同一模型中,Fimepinostat 比 GDC-0941、SAHA 或这两种化合物以最大耐受剂量 (MTD) 的组合获得更好的疗效。此外,在 SU-DHL4 弥漫性大 B 细胞淋巴瘤 (DLBCL) 的异种移植肿瘤模型中,Fimepinostat 在静脉内 (50 mg/kg) 或口服给药 (100 mg/kg) 后导致肿瘤消退或停滞,并导致 KRAS-突变体 A549 NSCLC 异种移植细胞[1]

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

    Clinical Trial
    分子量

    508.55

    Formula

    C23H24N8O4S

    CAS 号
    性状

    固体

    颜色

    White to light yellow

    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 : 43.75 mg/mL (86.03 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    DMF 中的溶解度 : 5 mg/mL (9.83 mM; 超声助溶)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9664 mL 9.8319 mL 19.6637 mL
    5 mM 0.3933 mL 1.9664 mL 3.9328 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: ≥ 2.08 mg/mL (4.09 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (4.09 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

    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: 30% SBE-β-CD in Saline

      Solubility: 10 mg/mL (19.66 mM); 悬浊液; 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
    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: 99.95%

    参考文献
    Kinase Assay
    [1]

    The activities of classes I and II HDACs are measured using the Color-de-Lys assay system. The activity of PI3K is measured using the ADP-Glo luminescent kinase assay. Recombinant PI3K protein, a complex of N-terminal GST-tagged recombinant full-length human p110 and untagged recombinant full-length human p85, is coexpressed in a baculovirus-infected Sf9 cell expression system[1].

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

    Cell Assay
    [1]

    Human cancer cell lines are plated at densities of 5,000 to 10,000 per well in 96-well flat-bottomed plates with the recommended culture medium. The cells are then incubated with compounds (e.g.,Fimepinostat) at various concentrations for 72 hours in culture medium supplemented with 0.5% (v/v) FBS. Growth inhibition is assessed by assay of cellular ATP content using the Perkin-Elmer ATPlite kit[1].

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

    Animal Administration
    [1]

    Mice[1]
    Six- to 8-week-old female athymic (nude nu/nu CD-1) or severe combined immunodeficient (SCID) mice obtained from Charles River Laboratories are injected subcutaneously with 3 to 20×106 cells in a medium suspension of 100 to 200 μL into the right hind flank region. Varying doses of Fimepinostat, standard anticancer agents, or vehicle are administered orally or via tail vein injection as indicated.

    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, 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
    DMF / DMSO 1 mM 1.9664 mL 9.8319 mL 19.6638 mL 49.1594 mL
    5 mM 0.3933 mL 1.9664 mL 3.9328 mL 9.8319 mL
    DMSO 10 mM 0.1966 mL 0.9832 mL 1.9664 mL 4.9159 mL
    15 mM 0.1311 mL 0.6555 mL 1.3109 mL 3.2773 mL
    20 mM 0.0983 mL 0.4916 mL 0.9832 mL 2.4580 mL
    25 mM 0.0787 mL 0.3933 mL 0.7866 mL 1.9664 mL
    30 mM 0.0655 mL 0.3277 mL 0.6555 mL 1.6386 mL
    40 mM 0.0492 mL 0.2458 mL 0.4916 mL 1.2290 mL
    50 mM 0.0393 mL 0.1966 mL 0.3933 mL 0.9832 mL
    60 mM 0.0328 mL 0.1639 mL 0.3277 mL 0.8193 mL
    80 mM 0.0246 mL 0.1229 mL 0.2458 mL 0.6145 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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    产品名称:
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