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

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 分別為 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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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥893
In-stock
1 mg ￥363
In-stock
5 mg ￥798
In-stock
10 mg ￥1244
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25 mg ￥2350
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50 mg ￥3663
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100 mg ￥5094
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500 mg 現(xiàn)貨 詢(xún)價(jià)
1 g   詢(xún)價(jià)  
5 g   詢(xún)價(jià)  

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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

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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)

    細(xì)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]
    體外研究
    (In Vitro)

    Fimepinostat 是一種有效的 HDAC I 類(lèi)和 II 類(lèi)酶泛抑制劑，觀察到它對(duì) I 類(lèi) HDAC 的效力與 LBH589 相似，但高于 SAHA。Fimepinostat 也是 I 類(lèi) PI3K 激酶的有效抑制劑，對(duì) PI3Kα、PI3Kβ 和 PI3Kδ 的 IC50 分別為 19、54 和 39 nM。Fimepinostat 顯著誘導(dǎo) H460 中的 p21 蛋白，H460 是一種非小細(xì)胞肺癌 (NSCLC) 細(xì)胞系。Fimepinostat 導(dǎo)致 RPMI-8226 多發(fā)性骨髓瘤細(xì)胞中 p-STAT3 (Y-705) 和 p-SRC 的減少，并降低 H1975 NSCLC 細(xì)胞和 BT-分別為 474 個(gè)乳腺癌細(xì)胞。Fimepinostat 以劑量依賴(lài)性方式誘導(dǎo) HCT-116 結(jié)腸癌細(xì)胞中的 caspase-3 和-7 激活。Fimepinostat 有效抑制源自血液腫瘤和實(shí)體瘤的癌細(xì)胞的生長(zhǎng)。Fimepinostat 有效抑制表達(dá)突變型或野生型 PI3K 的細(xì)胞的增殖[1]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    口服 Fimepinostat 以劑量依賴(lài)性方式抑制 Daudi 癌細(xì)胞異種移植物的生長(zhǎng)。在該模型中觀察到 100 mg/kg 的腫瘤停滯而沒(méi)有明顯的毒性。重要的是，在同一模型中，F(xiàn)imepinostat 比 GDC-0941、SAHA 或這兩種化合物以最大耐受劑量 (MTD) 的組合獲得更好的療效。此外，在 SU-DHL4 彌漫性大 B 細(xì)胞淋巴瘤 (DLBCL) 的異種移植腫瘤模型中，F(xiàn)imepinostat 在靜脈內(nèi) (50 mg/kg) 或口服給藥 (100 mg/kg) 后導(dǎo)致腫瘤消退或停滯，并導(dǎo)致 KRAS-突變體 A549 NSCLC 異種移植細(xì)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 號(hào)
    性狀

    固體

    顏色

    White to light yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 43.75 mg/mL (86.03 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

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

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

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    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

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

      此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

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

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： 50% PEG300    50% Saline

      Solubility: 10 mg/mL (19.66 mM); 懸濁液; 超聲助溶

    • 方案 二

      請(qǐng)依序添加每種溶劑： 30% SBE-β-CD in Saline

      Solubility: 10 mg/mL (19.66 mM); 懸濁液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.95%

    參考文獻(xiàn)
    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.
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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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    Inquiry Information

    產(chǎn)品名稱(chēng)：
    Fimepinostat
    目錄號(hào)：
    HY-13522
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