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  1. Stem Cell/Wnt Autophagy
  2. Hedgehog Autophagy
  3. Vismodegib

Vismodegib  (Synonyms: 維莫德吉; GDC-0449)

目錄號(hào): HY-10440 純度: 99.95%
COA 產(chǎn)品使用指南 技術(shù)支持

Vismodegib (GDC-0449) 是一種具有口服活性的 hedgehog 抑制劑,IC50 值為 3 nM;還可抑制 P-gpABCG2 的活性,IC50 值分別為 3.0 μM 和 1.4 μM。

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Vismodegib Chemical Structure

Vismodegib Chemical Structure

CAS No. : 879085-55-9

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Customer Review

Other Forms of Vismodegib:

MCE 顧客使用本產(chǎn)品發(fā)表的 36 篇科研文獻(xiàn)

WB
IF

    Vismodegib purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 28;420:195-207.  [Abstract]

    Shh-Light 2 cells are transfected with Gli1 or Gli2 plasmids and the expression of proteins are analyzed by Western blot. Positive control JQ1, CBC and CBD inhibit Gli1 and Gli2 overexpression induced Gli luciferase activity, GDC-0499 and GANT61 have no effects.

    Vismodegib purchased from MCE. Usage Cited in: Oncogenesis. 2018 Mar 13;7(3):24.  [Abstract]

    786-O and ACHN tumorspheres are treated with 0.1% CSE with/without 10 mM Vismodegib for 5 days. Western blotting analysis of SHH pathway proteins.

    Vismodegib purchased from MCE. Usage Cited in: J Genet Genomics. 2018 May 20;45(5):237-246.  [Abstract]

    Drug-feeding scheme (upper panel). Memory rescuing effects through treatment with LDE225 (LDE) or Vismodegib (VIS) at 20 mg/kg for 7.5-m-old and 15-m-old mice (lower panel, n=7 for each group).

    Vismodegib purchased from MCE. Usage Cited in: Anticancer Drugs. 2018 Mar;29(3):208-215.  [Abstract]

    SUM159 sphereforming cells are treated with 15 μM XAV-939 for 7 days, and the protein expression levels of breast cancer stem cells (CSCs) markers are detected by western blotting.

    Vismodegib purchased from MCE. Usage Cited in: Anticancer Drugs. 2018 Mar;29(3):208-215.  [Abstract]

    SUM159 sphere-forming cells are treated with Vismodegib (15 μM), a Smoothened (Smo) inhibitor for 7 days, and the protein expression levels of breast cancer stem cells (CSCs) play markers are detected by western blotting.

    Vismodegib purchased from MCE. Usage Cited in: Dev Neurobiol. 2017 Dec;77(12):1385-1400.  [Abstract]

    Reducing Shh signaling through Vismodegib treatment in Xenopus results in a significant rostral expansion of hypaxial muscle fibers.
    • 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

    Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively[1][2].

    IC50 & Target

    IC50: 3 nM (hedgehog), 3.0 μM (P-gp), 1.4 μM (ABCG2)[1][2]

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    > 100 μM
    Compound: VIS; GDC-0449
    Antiproliferation activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferation activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 32690258]
    AN3-CA IC50
    93 μM
    Compound: VIS; GDC-0449
    Antiproliferation activity against human AN3CA cells assessed as reduction in cell viability incubated for 72 hr by MTT assay
    Antiproliferation activity against human AN3CA cells assessed as reduction in cell viability incubated for 72 hr by MTT assay
    [PMID: 32690258]
    BXPC-3 IC50
    47.95 μM
    Compound: 1; GDC-0449
    Antiproliferative activity against human BxPC3 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
    Antiproliferative activity against human BxPC3 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
    [PMID: 26820554]
    C3H 10T1/2 IC50
    0.011 μM
    Compound: GDC-0449
    Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs
    Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs
    [PMID: 22268551]
    C3H 10T1/2 IC50
    0.013 μM
    Compound: 31, GDC-0449
    Inhibition of SHH in mouse C3H10T1/2 cells by Gli-luciferase reporter gene assay
    Inhibition of SHH in mouse C3H10T1/2 cells by Gli-luciferase reporter gene assay
    [PMID: 19716296]
    C3H 10T1/2 IC50
    0.017 μM
    Compound: Vismodegib
    Inhibition of hedgehog signalling in mouse C3H10T1/2 cells assessed as reduction in Smo agonist SAG induced cell differentiation into alkaline phosphatase-positive osteoblasts using pNp substrate incubated for 72 hrs
    Inhibition of hedgehog signalling in mouse C3H10T1/2 cells assessed as reduction in Smo agonist SAG induced cell differentiation into alkaline phosphatase-positive osteoblasts using pNp substrate incubated for 72 hrs
    10.1039/C5MD00092K
    C3H 10T1/2 EC50
    4.7 nM
    Compound: 1
    Inhibition of SMO-mediated Hedgehog signaling pathway in mouse C3H10T1/2 cells assessed as reduction in sonic hedgehog-induced osteoblast differentiation by measuring alkaline phosphatase activity incubated for 72 hrs
    Inhibition of SMO-mediated Hedgehog signaling pathway in mouse C3H10T1/2 cells assessed as reduction in sonic hedgehog-induced osteoblast differentiation by measuring alkaline phosphatase activity incubated for 72 hrs
    [PMID: 31862310]
    C3H 10T1/2 IC50
    5 nM
    Compound: GDC-0449
    Inhibition of Smo in mouse C3H10T1/2 cells using human recombinant SHH assessed as effect on SMO/SHH transient transcriptional activation after 20 hrs by Gli-luciferase reporter assay
    Inhibition of Smo in mouse C3H10T1/2 cells using human recombinant SHH assessed as effect on SMO/SHH transient transcriptional activation after 20 hrs by Gli-luciferase reporter assay
    [PMID: 24900436]
    CCRF-CEM IC50
    58 μM
    Compound: 17
    Antiproliferative activity against human CEM cells incubated for 96 hrs by Coulter counter method
    Antiproliferative activity against human CEM cells incubated for 96 hrs by Coulter counter method
    [PMID: 32686940]
    Daoy IC50
    0.086 μM
    Compound: 1, GDC-0449
    Inhibition of Hedgehog signaling in human DaOY cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by RT-PCR analysis
    Inhibition of Hedgehog signaling in human DaOY cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by RT-PCR analysis
    [PMID: 24900716]
    HEK293 IC50
    0.0051 μM
    Compound: 54
    Displacement of BODIPY-cyclopamine from human Smo expressed in HEK293 cells incubated for 3 hrs by fluorescence competitive displacement assay
    Displacement of BODIPY-cyclopamine from human Smo expressed in HEK293 cells incubated for 3 hrs by fluorescence competitive displacement assay
    10.1039/C6MD00020G
    HEK293 IC50
    0.006 μM
    Compound: Vismodegib
    Displacement of boron-dipyrromethene-cyclopamine from human smoothened receptor expressed in HEK293 cells incubated for 4 hrs by hSMO-BC binding assay
    Displacement of boron-dipyrromethene-cyclopamine from human smoothened receptor expressed in HEK293 cells incubated for 4 hrs by hSMO-BC binding assay
    10.1039/C5MD00092K
    HEK293 IC50
    7 nM
    Compound: GDC-0449
    Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy
    Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy
    [PMID: 22268551]
    HeLa EC50
    0.002 μM
    Compound: 1
    Displacement of BODIPY-labeled cyclopamine from mouse SMO transfected in human HeLa cells by competition binding assay
    Displacement of BODIPY-labeled cyclopamine from mouse SMO transfected in human HeLa cells by competition binding assay
    [PMID: 31862310]
    HeLa EC50
    0.003 μM
    Compound: 1
    Displacement of BODIPY-labeled cyclopamine from human SMO transfected in human HeLa cells by competition binding assay
    Displacement of BODIPY-labeled cyclopamine from human SMO transfected in human HeLa cells by competition binding assay
    [PMID: 31862310]
    HeLa IC50
    61.7 μM
    Compound: VIS; GDC-0449
    Antiproliferation activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferation activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 32690258]
    HeLa IC50
    64 μM
    Compound: 17
    Antiproliferative activity against human HeLa cells incubated for 4 days by Coulter counter method
    Antiproliferative activity against human HeLa cells incubated for 4 days by Coulter counter method
    [PMID: 32686940]
    HMEC-1 IC50
    41 μM
    Compound: 17
    Growth inhibition of HMEC-1 incubated for 4 days by Coulter counter method
    Growth inhibition of HMEC-1 incubated for 4 days by Coulter counter method
    [PMID: 32686940]
    HT-1080 IC50
    > 100 μM
    Compound: GDC-0449; 1
    Antiproliferative activity against human HT1080 cells after 72 hrs by sulforhodamine-B assay
    Antiproliferative activity against human HT1080 cells after 72 hrs by sulforhodamine-B assay
    [PMID: 30099257]
    HT-29 IC50
    1.08 μM
    Compound: Vismodegib
    Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    10.1039/C5MD00092K
    L1210 IC50
    49 μM
    Compound: 17
    Antiproliferative activity against mouse L1210 cells incubated for 48 hrs by Coulter counter method
    Antiproliferative activity against mouse L1210 cells incubated for 48 hrs by Coulter counter method
    [PMID: 32686940]
    LS174T IC50
    45.81 μM
    Compound: 1; GDC-0449
    Antiproliferative activity against human LS174T cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
    Antiproliferative activity against human LS174T cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
    [PMID: 26820554]
    LS180 IC50
    45 μM
    Compound: GDC-0449; 1
    Antiproliferative activity against human LS180 cells after 72 hrs by sulforhodamine-B assay
    Antiproliferative activity against human LS180 cells after 72 hrs by sulforhodamine-B assay
    [PMID: 30099257]
    MCF-10A IC50
    89.5 μM
    Compound: VIS; GDC-0449
    Cytotoxicity against human MCF10A cells assessed as cell viability incubated for 72 hrs measured by MTT assay
    Cytotoxicity against human MCF10A cells assessed as cell viability incubated for 72 hrs measured by MTT assay
    [PMID: 32690258]
    MCF7 IC50
    > 100 μM
    Compound: VIS; GDC-0449
    Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 32690258]
    MCF7 IC50
    > 50 μM
    Compound: Vismodegib
    Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
    [PMID: 29107429]
    MDA-MB-231 IC50
    > 100 μM
    Compound: VIS; GDC-0449
    Antiproliferation activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs measured after 4 hrs by MTT assay
    Antiproliferation activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs measured after 4 hrs by MTT assay
    [PMID: 32690258]
    MDA-MB-231 IC50
    > 50 μM
    Compound: Vismodegib
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
    [PMID: 29107429]
    MDA-MB-468 IC50
    79 μM
    Compound: VIS; GDC-0449
    Antiproliferation activity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hr by MTT assay
    Antiproliferation activity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hr by MTT assay
    [PMID: 32690258]
    Medulloblastoma cell IC50
    30.4 nM
    Compound: 1; GDC-0449
    Antiproliferative activity against Ptch+/- and p53-/- mouse medulloblastoma cells after 36 hrs by Brdu incorporation assay
    Antiproliferative activity against Ptch+/- and p53-/- mouse medulloblastoma cells after 36 hrs by Brdu incorporation assay
    [PMID: 28688278]
    Medulloblastoma cell IC50
    4.7 nM
    Compound: GDC-0449
    Antiproliferative activity against mouse Ptch+/- medulloblastoma cells assessed as inhibition of cell growth incubated for 36 hrs by CCK-8 assay
    Antiproliferative activity against mouse Ptch+/- medulloblastoma cells assessed as inhibition of cell growth incubated for 36 hrs by CCK-8 assay
    [PMID: 30939349]
    MGC-803 IC50
    2.39 μM
    Compound: Vismodegib
    Antiproliferative activity against human MGC803 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    Antiproliferative activity against human MGC803 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    10.1039/C5MD00092K
    NIH3T3 IC50
    0.023 μM
    Compound: GDC-0449
    Inhibition of Smo receptor (unknown origin) expressed in NIH3T3 cells assessed as inhibition of Smo agonist SAG-induced GRE activation after 30 hrs by luciferase reporter gene assay
    Inhibition of Smo receptor (unknown origin) expressed in NIH3T3 cells assessed as inhibition of Smo agonist SAG-induced GRE activation after 30 hrs by luciferase reporter gene assay
    [PMID: 24726807]
    NIH3T3 IC50
    0.025 μM
    Compound: 54
    Inhibition of Hh receptor (unknown origin) expressed in SAG-stimulated mouse NIH3T3 cells incubated for 24 hrs by Gli-luciferase reporter gene assay
    Inhibition of Hh receptor (unknown origin) expressed in SAG-stimulated mouse NIH3T3 cells incubated for 24 hrs by Gli-luciferase reporter gene assay
    10.1039/C6MD00020G
    NIH3T3 IC50
    7.17 nM
    Compound: GDC-0449
    Inhibition of hedgehog receptor signaling pathway in mouse NIH3T3 cells transfected with Gli-reporter gene by luciferase reporter gene assay
    Inhibition of hedgehog receptor signaling pathway in mouse NIH3T3 cells transfected with Gli-reporter gene by luciferase reporter gene assay
    [PMID: 24923765]
    NIH3T3 IC50
    7.2 nM
    Compound: 1; GDC-0449
    Inhibition of hedgehog signalling in mouse NIH3T3 cells stably transfected with Gli-luciferase construct incubated for 48 hrs by dual luciferase reporter gene assay
    Inhibition of hedgehog signalling in mouse NIH3T3 cells stably transfected with Gli-luciferase construct incubated for 48 hrs by dual luciferase reporter gene assay
    [PMID: 26827136]
    NIH3T3 IC50
    7.2 nM
    Compound: 1; GDC-0449
    Inhibition of Sonic-induced hedgehog signalling in mouse NIH3T3 cells after 48 hrs by Gli-luciferase reporter assay
    Inhibition of Sonic-induced hedgehog signalling in mouse NIH3T3 cells after 48 hrs by Gli-luciferase reporter assay
    [PMID: 26820554]
    NIH3T3 IC50
    7.2 nM
    Compound: GDC-0449
    Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells after 48 hrs by Gli-luciferase reporter gene assay
    Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells after 48 hrs by Gli-luciferase reporter gene assay
    [PMID: 24486203]
    NIH3T3 IC50
    7.2 nM
    Compound: GDC-0449, vismodegib
    Inhibition of SHH signaling pathway in mouse NIH3T3 cells measured after 48 hrs by Gli-luciferase reporter assay
    Inhibition of SHH signaling pathway in mouse NIH3T3 cells measured after 48 hrs by Gli-luciferase reporter assay
    [PMID: 24176396]
    NIH3T3 IC50
    7.2 nM
    Compound: GDC, GDC-0449
    Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells by Gli1-luciferase reporter gene assay
    Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells by Gli1-luciferase reporter gene assay
    [PMID: 24405704]
    PC-3 IC50
    > 50 μM
    Compound: Vismodegib
    Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
    Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
    [PMID: 29107429]
    PC-3 IC50
    66.78 μM
    Compound: 1; GDC-0449
    Antiproliferative activity against human PC3 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
    Antiproliferative activity against human PC3 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
    [PMID: 26820554]
    Shh Light II IC50
    0.007 μM
    Compound: GDC-0449
    Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay
    Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay
    [PMID: 22268551]
    Shh Light II IC50
    1.5 nM
    Compound: GDC-0449
    Antagonist activity at Smo in mouse Shh-Light 2 cells assessed as inhibition of Shh-induced Gli1-reporter activity after 2 days by dual-luciferase reporter gene method
    Antagonist activity at Smo in mouse Shh-Light 2 cells assessed as inhibition of Shh-induced Gli1-reporter activity after 2 days by dual-luciferase reporter gene method
    [PMID: 23063522]
    Shh Light II IC50
    3 nM
    Compound: 101, GDC-0449
    Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay
    Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay
    [PMID: 19309080]
    Shh Light II IC50
    33 nM
    Compound: GDC-0449
    Antagonist activity at smoothened (unknown origin) expressed in mouse Shh Light2 cells co-expressing Gli-dependent reporter gene assessed as inhibition of Hh signaling by dual luciferase reporter gene assay
    Antagonist activity at smoothened (unknown origin) expressed in mouse Shh Light2 cells co-expressing Gli-dependent reporter gene assessed as inhibition of Hh signaling by dual luciferase reporter gene assay
    [PMID: 24491459]
    SW-620 IC50
    10.92 μM
    Compound: Vismodegib
    Antiproliferative activity against human SW620 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    Antiproliferative activity against human SW620 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    10.1039/C5MD00092K
    T47D IC50
    > 100 μM
    Compound: VIS; GDC-0449
    Antiproliferation activity against human T47D cells assessed as reduction in cell viability incubated for 72 hr by MTT assay
    Antiproliferation activity against human T47D cells assessed as reduction in cell viability incubated for 72 hr by MTT assay
    [PMID: 32690258]
    T47D IC50
    41.34 μM
    Compound: Vismodegib
    Cytotoxicity against human T47D cells after 72 hrs by MTT assay
    Cytotoxicity against human T47D cells after 72 hrs by MTT assay
    [PMID: 29107429]
    U-251 IC50
    > 100 μM
    Compound: VIS; GDC-0449
    Antiproliferation activity against human U251 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferation activity against human U251 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 32690258]
    U2OS IC50
    74 nM
    Compound: GDC-0449
    Displacement of BODIPY-Cyclopamine from human HA-tagged Smo receptor expressed in human U2OS cells at 1 to 10000 nM incubated for 2 hrs by DAPI staining based fluorescence microscopic method
    Displacement of BODIPY-Cyclopamine from human HA-tagged Smo receptor expressed in human U2OS cells at 1 to 10000 nM incubated for 2 hrs by DAPI staining based fluorescence microscopic method
    [PMID: 30939349]
    體外研究
    (In Vitro)

    Vismodegib (HhAntag691) 是一種 ABCG2 抑制劑,可通過阻斷 HEK293 細(xì)胞中 NSC 279836 (另一種 ABCG2 底物) 的輸出來增加其有效細(xì)胞內(nèi)濃度。Vismodegib (HhAntag691,10 μM),使 MDCKII/Pgp 細(xì)胞和 MDCKII/MRP1 細(xì)胞對 NSC757 處理重新敏感[2]
    Vismodegib (25 μM 或 50 μM) 濃度依賴性地抑制 HCC 和 H1339 細(xì)胞[3]。

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

    體內(nèi)研究
    (In Vivo)

    Vismodegib (0.3 to 75 mg/kg,po) 在髓母細(xì)胞瘤同種異體移植腫瘤中非常有效。Vismodegib (> 46 mg/kg,口服) 導(dǎo)致患者來源的結(jié)直腸異種移植物生長延遲[4]

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

    Clinical Trial
    分子量

    421.30

    Formula

    C19H14Cl2N2O3S

    CAS 號(hào)
    性狀

    固體

    顏色

    Off-white to light yellow

    中文名稱

    維莫德吉

    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 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : 50 mg/mL (118.68 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

    Ethanol 中的溶解度 : 3.33 mg/mL (7.90 mM; 超聲助溶 (<60°C))

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.3736 mL 11.8681 mL 23.7362 mL
    5 mM 0.4747 mL 2.3736 mL 4.7472 mL
    查看完整儲(chǔ)備液配制表

    * 請根據(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, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí),請?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請?jiān)?個(gè)月內(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

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn):

    請根據(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;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.93 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 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

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

      Solubility: 2.5 mg/mL (5.93 mM); 懸濁液; 超聲加熱助溶

      此方案可獲得 2.5 mg/mL的均勻懸濁液,懸濁液可用于口服和腹腔注射。

      1 mL 工作液為例,取 100 μL 25.0 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。
    動(dòng)物溶解方案計(jì)算器
    請輸入動(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

    由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
    請輸入您的動(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 2%。
    方案所需 助溶劑 包括:DMSO ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
    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)備液濃度超過該產(chǎn)品的實(shí)測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(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)給藥周期超過半月以上,請謹(jǐn)慎選擇該方案。
    請確保第一步儲(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: 99.97%

    參考文獻(xiàn)
    Cell Assay
    [2]

    When MTT assay is performed, an MTT reagent is added to each well to a final concentration of 150 μg/mL, and the cells are incubated for 1 to 2 hours at 37°C. The medium is then replaced with DMSO to dissolve the reaction product. Absorbance at 570 nm is quantified using a spectra MAX 340pc plate reader. For the XTT assay, 1 mg/mL XTT is mixed with 0.025 mM PMS, and 50 μL of the mixture is added to each well and incubated for 4 hours at 37°C. After the plates are mixed on a plate shaker, absorbance at 450 nm is measured. All results are normalized to a percentage of absorbance obtained in controls.

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

    Animal Administration
    [2]

    Tumor-bearing mice are distributed into tumor volume-matched cohorts when the tumors reache between 200 and 350 mm3. The vismodegib-resistant medulloblastoma allograft, sg274, is developed by intermittent suboptimal dosing of a?Ptch+/?, p53?/?medulloblastoma allograft. Vismodegib is formulated as a suspension in 0.5% methyl-cellulose, 0.2% tween-80 (MCT), and is administered orally. Tumor volumes are determined using digital calipers using the formula (L×W×W)/2. Tumor growth inhibition (%TGI) is calculated as the percentage of the area under the fitted curve (AUC) for the respective dose group per day in relation to the vehicle, such that %TGI=100×1-(AUCtreatment/day)/(AUCvehicle/day).

    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, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí),請?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 2.3736 mL 11.8681 mL 23.7362 mL 59.3406 mL
    5 mM 0.4747 mL 2.3736 mL 4.7472 mL 11.8681 mL
    DMSO 10 mM 0.2374 mL 1.1868 mL 2.3736 mL 5.9341 mL
    15 mM 0.1582 mL 0.7912 mL 1.5824 mL 3.9560 mL
    20 mM 0.1187 mL 0.5934 mL 1.1868 mL 2.9670 mL
    25 mM 0.0949 mL 0.4747 mL 0.9494 mL 2.3736 mL
    30 mM 0.0791 mL 0.3956 mL 0.7912 mL 1.9780 mL
    40 mM 0.0593 mL 0.2967 mL 0.5934 mL 1.4835 mL
    50 mM 0.0475 mL 0.2374 mL 0.4747 mL 1.1868 mL
    60 mM 0.0396 mL 0.1978 mL 0.3956 mL 0.9890 mL
    80 mM 0.0297 mL 0.1484 mL 0.2967 mL 0.7418 mL
    100 mM 0.0237 mL 0.1187 mL 0.2374 mL 0.5934 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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