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  1. Cell Cycle/DNA Damage Autophagy Apoptosis
  2. DNA Alkylator/Crosslinker Autophagy Apoptosis
  3. Temozolomide

Temozolomide  (Synonyms: 替莫唑胺; NSC 362856; CCRG 81045; TMZ)

目錄號: HY-17364 純度: 99.96%
COA 產(chǎn)品使用指南 技術支持

Temozolomide (NSC 362856) 是一種可透過血腦屏障的口服活性的 DNA 烷基化 (DNA alkylating) 劑。Temozolomide 也是一種促自噬 (autophagy) 和促凋亡劑 (apoptosis)。Temozolomide 對以低水平的 O6-烷基鳥嘌呤 DNA 烷基轉移酶 (OGAT) 和功能失配修復系統(tǒng)為特征的腫瘤細胞有效。Temozolomide 具有抗腫瘤和抗血管生成作用。

MCE 的所有產(chǎn)品僅用作科學研究或藥證申報,我們不為任何個人用途提供產(chǎn)品和服務

Temozolomide Chemical Structure

Temozolomide Chemical Structure

CAS No. : 85622-93-1

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Other Forms of Temozolomide:

MCE 顧客使用本產(chǎn)品發(fā)表的 121 篇科研文獻

Proliferation Assay
WB
Cell Viability Assay
IF

    Temozolomide purchased from MCE. Usage Cited in: Oncogene. 2023 Mar 7.  [Abstract]

    Temozolomide (TMZ; 60 mg/kg, i.g.; 5 consecutive days) treatment individually can suppress tumor growth, and the combination of knockdown MAEA and TMZ treatment can significantly inhibit tumor growth in mice (Fig A-B).

    Temozolomide purchased from MCE. Usage Cited in: J Pharm Anal. 2023 Apr 19.

    Temozolomide (TMZ; 10 μM; 24 h) enhances the Sunitinib-induced (3 μM; 24 h) expression of γ-H2Ax in T98G cells.

    Temozolomide purchased from MCE. Usage Cited in: J Pharm Anal. 2023 Apr 19.

    Temozolomide (TMZ; 10 μM; 24 h) enhances the Sunitinib-induced (3 μM; 24 h) expression of γ-H2Ax in T98G cells.

    Temozolomide purchased from MCE. Usage Cited in: Front Cell Dev Biol. 2021 Feb 1;9:620883.  [Abstract]

    Analyses of Western blotting shows that Temozolomide (TMZ) treatment increases the expression of CD133, SOX2, OCT4, and NANOG, suggesting that TMZ treatment promotes glioma stem cells (GSCs) formation in GBM cells.

    Temozolomide purchased from MCE. Usage Cited in: Oncotarget. 2016 May 17;7(20):29116-30.  [Abstract]

    U87MG glioma cells, and GBM8401 glioma cells are treated with DMSO or 20, 40, 60, or 80 μM of Hono, Mag or Hono-Mag combination for 24 hours. After treatment, the survival rate is analyzed using MTT tests. The right panels show Temozolomide (TMZ)-treated glioma cells which are regarded as a positive control.
    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects[1][2].

    IC50 & Target

    DNA alkylator[1]

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A 172 IC50
    > 40 μM
    Compound: TMZ
    Cytotoxicity against human A 172 cells assessed as cell viability measured after 96 hrs by XTT assay
    Cytotoxicity against human A 172 cells assessed as cell viability measured after 96 hrs by XTT assay
    [PMID: 34507011]
    A 172 IC50
    6.5 x 104 nM
    Compound: Temozolamide
    Antiproliferative activity against human A172 cells after 5 days by MTT assay
    Antiproliferative activity against human A172 cells after 5 days by MTT assay
    [PMID: 22608389]
    A2058 IC50
    35.5 μM
    Compound: 1, TMZ
    Chemosensitization of human A2058 cells after 5 days by MTT assay
    Chemosensitization of human A2058 cells after 5 days by MTT assay
    [PMID: 23895620]
    A2780 IC50
    > 250 μM
    Compound: 1, TMZ
    Chemosensitization of human A2780 cells after 5 days by MTT assay
    Chemosensitization of human A2780 cells after 5 days by MTT assay
    [PMID: 23895620]
    A2780 IC50
    > 250 μM
    Compound: 1, TMZ
    Cytotoxicity against human A2780 cells after 5 days by MTT assay in presence of 10 uM MGMT inactivator Patrin2
    Cytotoxicity against human A2780 cells after 5 days by MTT assay in presence of 10 uM MGMT inactivator Patrin2
    [PMID: 24900418]
    A2780 IC50
    368 μM
    Compound: Temozolomide
    Potentiation of growth inhibition of A2780 cells by compound alone in experiment 2
    Potentiation of growth inhibition of A2780 cells by compound alone in experiment 2
    [PMID: 11063605]
    A2780 IC50
    525 μM
    Compound: Temozolomide
    Potentiation of growth inhibition of A2780 by compound alone in experiment 1
    Potentiation of growth inhibition of A2780 by compound alone in experiment 1
    [PMID: 11063605]
    A2780 IC50
    8.5 μM
    Compound: 1, TMZ
    Chemosensitization of human A2780 cells after 5 days by MTT assay in presence of MGMT inactivator PaTrin2
    Chemosensitization of human A2780 cells after 5 days by MTT assay in presence of MGMT inactivator PaTrin2
    [PMID: 23895620]
    A-375 IC50
    > 75 μM
    Compound: TMZ
    Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    [PMID: 34795855]
    A-431 IC50
    366 μM
    Compound: TEM
    Antiproliferative activity in human A431 Cells after 72 hrs by SRB assay
    Antiproliferative activity in human A431 Cells after 72 hrs by SRB assay
    [PMID: 28494256]
    A549 IC50
    > 250 μM
    Compound: 1, TMZ
    Cytotoxicity against human A549 cells after 5 days by MTT assay
    Cytotoxicity against human A549 cells after 5 days by MTT assay
    [PMID: 24900418]
    Astrocyte IC50
    > 1 mM
    Compound: Temozolamide
    Cytotoxicity against mouse primary astrocytes after 5 days by MTT assay
    Cytotoxicity against mouse primary astrocytes after 5 days by MTT assay
    [PMID: 22608389]
    Astrocyte EC50
    51.8 μM
    Compound: 3, TMZ
    Cytotoxicity against Rattus norvegicus Sprague-Dawley (rat) astrocytes after 4 days by cresylecth violet-staining method
    Cytotoxicity against Rattus norvegicus Sprague-Dawley (rat) astrocytes after 4 days by cresylecth violet-staining method
    10.1007/s00044-010-9356-8
    B16-F10 IC50
    > 75 μM
    Compound: TMZ
    Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    [PMID: 34795855]
    B16-F10 IC50
    > 75 μM
    Compound: Temozolomide
    Cytotoxicity against mouse B16F10 cells after 72 hrs by MTS assay
    Cytotoxicity against mouse B16F10 cells after 72 hrs by MTS assay
    [PMID: 28602669]
    B16-F10 IC50
    258 μM
    Compound: Temozolomide
    Growth inhibition of mouse B16F10 cells after 72 hrs by MTT assay
    Growth inhibition of mouse B16F10 cells after 72 hrs by MTT assay
    [PMID: 22809560]
    C6 IC50
    > 30 μM
    Compound: TMZ
    Antiproliferative activity against rat C6 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against rat C6 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 34656900]
    C6 EC50
    16.5 μM
    Compound: 3, TMZ
    Cytotoxicity against Rattus norvegicus (rat) C6 cells after 4 days by cresylecth violet-staining method
    Cytotoxicity against Rattus norvegicus (rat) C6 cells after 4 days by cresylecth violet-staining method
    10.1007/s00044-010-9356-8
    C6 IC50
    34 μM
    Compound: Temozolomide
    Cytotoxicity against rat C6 cells incubated for 48 hrs by MTT assay
    Cytotoxicity against rat C6 cells incubated for 48 hrs by MTT assay
    [PMID: 23069682]
    C6 EC50
    60.46 μM
    Compound: TMZ
    Antiproliferative activity against rat C6 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    Antiproliferative activity against rat C6 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    [PMID: 31978780]
    C6 IC50
    60.46 μM
    Compound: TMZ
    Inhibition of cell proliferation of rat C6 cells assessed as cell viability after 72 hrs by sulforhodamine B assay
    Inhibition of cell proliferation of rat C6 cells assessed as cell viability after 72 hrs by sulforhodamine B assay
    [PMID: 25442304]
    CTX TNA2 IC50
    430.6 μM
    Compound: TMZ
    Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 32960603]
    CTX TNA2 IC50
    486.9 μM
    Compound: TMZ
    Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 32960603]
    CTX TNA2 IC50
    666.4 μM
    Compound: TMZ
    Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    [PMID: 32960603]
    DBTRG-05MG IC50
    119.3 μM
    Compound: TMZ
    Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 32960603]
    DBTRG-05MG IC50
    354.7 μM
    Compound: TMZ
    Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 32960603]
    DBTRG-05MG IC50
    973.9 μM
    Compound: TMZ
    Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 24 hrs by MTT assay
    [PMID: 32960603]
    DLD-1 IC50
    > 250 μM
    Compound: 1, TMZ
    Cytotoxicity against human DLD1 cells after 5 days by MTT assay
    Cytotoxicity against human DLD1 cells after 5 days by MTT assay
    [PMID: 24900418]
    GL261 IC50
    > 100 μM
    Compound: TMZ
    Cytotoxicity against mouse GL261 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
    Cytotoxicity against mouse GL261 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
    [PMID: 30939350]
    H4 IC50
    > 100 μM
    Compound: TMZ
    Antiproliferative activity against human H4 cells after 48 hrs by MTT assay
    Antiproliferative activity against human H4 cells after 48 hrs by MTT assay
    [PMID: 26651221]
    HaCaT IC50
    > 75 μM
    Compound: TMZ
    Cytotoxicity against human HaCaT cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    Cytotoxicity against human HaCaT cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    [PMID: 34795855]
    HCT-116 IC50
    > 250 μM
    Compound: 1, TMZ
    Cytotoxicity against human HCT116 cells after 5 days by MTT assay
    Cytotoxicity against human HCT116 cells after 5 days by MTT assay
    [PMID: 24900418]
    HCT-116 IC50
    > 250 μM
    Compound: 1, TMZ
    Chemosensitization of human HCT116 cells after 5 days by MTT assay
    Chemosensitization of human HCT116 cells after 5 days by MTT assay
    [PMID: 23895620]
    HCT-116 IC50
    4.34 μM
    Compound: Temozolomide
    Cytotoxicity against human HCT116 cells after 4 days
    Cytotoxicity against human HCT116 cells after 4 days
    [PMID: 19800803]
    HeLa GI50
    > 50 μM
    Compound: TMZ
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 to 48 hrs by MTT assay
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 to 48 hrs by MTT assay
    [PMID: 24986661]
    Hs 683 IC50
    956 μM
    Compound: Temozolomide
    Growth inhibition of human Hs683 cells after 72 hrs by MTT assay
    Growth inhibition of human Hs683 cells after 72 hrs by MTT assay
    [PMID: 22809560]
    HT-29 IC50
    > 250 μM
    Compound: 1, TMZ
    Cytotoxicity against human HT-29 cells after 5 days by MTT assay
    Cytotoxicity against human HT-29 cells after 5 days by MTT assay
    [PMID: 24900418]
    LN-18 IC50
    3.9 x 105 nM
    Compound: Temozolamide
    Antiproliferative activity against human LN18 cells after 5 days by MTT assay
    Antiproliferative activity against human LN18 cells after 5 days by MTT assay
    [PMID: 22608389]
    LN-229 IC50
    67.81 μM
    Compound: TMZ
    Cytotoxicity effect against human LN-229 cells assessed as cell growth inhibition incubated for 48 hrs by trypan blue exclusion assay
    Cytotoxicity effect against human LN-229 cells assessed as cell growth inhibition incubated for 48 hrs by trypan blue exclusion assay
    [PMID: 34304559]
    LoVo IC50
    595 μM
    Compound: Temozolomide
    Cytotoxic potentiation of Topotecan (TP) by the compound in (human colorectal cancer LoVo cell line
    Cytotoxic potentiation of Topotecan (TP) by the compound in (human colorectal cancer LoVo cell line
    [PMID: 12408707]
    MDA-MB-238 IC50
    > 100 μM
    Compound: TMZ
    Cytotoxicity against human MDA-MB-238 cells assessed as cell viability measured after 96 hrs by XTT assay
    Cytotoxicity against human MDA-MB-238 cells assessed as cell viability measured after 96 hrs by XTT assay
    [PMID: 34507011]
    MDA-MB-436 IC50
    120 μM
    Compound: TMZ
    Growth inhibition of human MDA-MB-436 cells after 72 hrs by SRB assay
    Growth inhibition of human MDA-MB-436 cells after 72 hrs by SRB assay
    [PMID: 24388690]
    MDCK IC50
    > 1000 μM
    Compound: TMZ
    Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 72 hrs under normoxic condition by Alamar blue assay
    Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 72 hrs under normoxic condition by Alamar blue assay
    [PMID: 27823879]
    MDCK IC50
    > 1000 μM
    Compound: TMZ
    Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 72 hrs under hypoxic condition by Alamar blue assay
    Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 72 hrs under hypoxic condition by Alamar blue assay
    [PMID: 27823879]
    MDCK IC50
    1000 μM
    Compound: TMZ
    Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 72 hrs under hypoxic condition by Alamar blue assay
    Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 72 hrs under hypoxic condition by Alamar blue assay
    [PMID: 27823879]
    MDCK IC50
    775 μM
    Compound: TMZ
    Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 72 hrs under normoxic condition by Alamar blue assay
    Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 72 hrs under normoxic condition by Alamar blue assay
    [PMID: 27823879]
    NCI-H1299 IC50
    > 100 μM
    Compound: TMZ
    Cytotoxicity against human NCI-H1299 cells assessed as cell viability measured after 96 hrs by XTT assay
    Cytotoxicity against human NCI-H1299 cells assessed as cell viability measured after 96 hrs by XTT assay
    [PMID: 34507011]
    PANC-1 IC50
    > 250 μM
    Compound: 1, TMZ
    Cytotoxicity against human PANC1 cells after 5 days by MTT assay
    Cytotoxicity against human PANC1 cells after 5 days by MTT assay
    [PMID: 24900418]
    Panel NCI-60 cells GI50
    > 100 μM
    Compound: 1; TMZ
    Growth inhibition of human NCI60 cells after 48 hrs by MTT assay
    Growth inhibition of human NCI60 cells after 48 hrs by MTT assay
    10.1039/C6MD00384B
    RG2 IC50
    106.7 μM
    Compound: TMZ
    Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 32960603]
    RG2 IC50
    348.2 μM
    Compound: TMZ
    Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 32960603]
    RG2 IC50
    962.5 μM
    Compound: TMZ
    Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    [PMID: 32960603]
    SH-SY5Y IC50
    > 100 μM
    Compound: TMZ
    Antiproliferative activity against human SH-SY5Y cells after 48 hrs by MTT assay
    Antiproliferative activity against human SH-SY5Y cells after 48 hrs by MTT assay
    [PMID: 26651221]
    SH-SY5Y IC50
    > 50 μM
    Compound: Temozolomide
    Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 29789258]
    SH-SY5Y IC50
    393 μM
    Compound: TMZ
    Cytotoxicity against human SH-SY5Y cells using best fit nonlinear regression analysis
    Cytotoxicity against human SH-SY5Y cells using best fit nonlinear regression analysis
    [PMID: 35044783]
    SH-SY5Y IC50
    512.62 μM
    Compound: TMZ
    Cytotoxicity against human SH-SY5Y cells assessed as cell viability using raw interpretation method
    Cytotoxicity against human SH-SY5Y cells assessed as cell viability using raw interpretation method
    [PMID: 35044783]
    SNB-19 IC50
    > 250 μM
    Compound: 1, TMZ
    Chemosensitization of human SNB19 cells expressing MGMT after 5 days by MTT assay
    Chemosensitization of human SNB19 cells expressing MGMT after 5 days by MTT assay
    [PMID: 23895620]
    SNB-19 GI50
    35.7 μM
    Compound: 1; TMZ
    Growth inhibition of vehicle-transfected human SNB19 cells after 7 days by MTT assay
    Growth inhibition of vehicle-transfected human SNB19 cells after 7 days by MTT assay
    [PMID: 30108945]
    SNB-19 IC50
    37 μM
    Compound: 1, TMZ
    Chemosensitization of MGMT-deficient human SNB19 cells after 5 days by MTT assay
    Chemosensitization of MGMT-deficient human SNB19 cells after 5 days by MTT assay
    [PMID: 23895620]
    SNB-19 GI50
    45.6 μM
    Compound: 1; TMZ
    Growth inhibition of empty vector transfected human SNB19 cells after 7 days by MTT assay
    Growth inhibition of empty vector transfected human SNB19 cells after 7 days by MTT assay
    10.1039/C6MD00384B
    SNB-19 GI50
    470 μM
    Compound: 1; TMZ
    Growth inhibition of MGMT-transfected human SNB19 cells expressing MGMT after 7 days by MTT assay
    Growth inhibition of MGMT-transfected human SNB19 cells expressing MGMT after 7 days by MTT assay
    [PMID: 30108945]
    SNB-19 GI50
    526 μM
    Compound: 1; TMZ
    Growth inhibition of MGMT-transfected human SNB19 cells after 7 days by MTT assay
    Growth inhibition of MGMT-transfected human SNB19 cells after 7 days by MTT assay
    10.1039/C6MD00384B
    SNB-19 IC50
    69.87 μM
    Compound: TMZ
    Cytotoxicity effect against human SNB-19 cells assessed as cell growth inhibition incubated for 48 hrs by trypan blue exclusion assay
    Cytotoxicity effect against human SNB-19 cells assessed as cell growth inhibition incubated for 48 hrs by trypan blue exclusion assay
    [PMID: 34304559]
    T98G GI50
    375 μM
    Compound: TMZ
    Antiproliferative activity against human T98G cells assessed as cell growth inhibition incubated for 96 hrs by CellTiter-Glo luminescent cell viability assay
    Antiproliferative activity against human T98G cells assessed as cell growth inhibition incubated for 96 hrs by CellTiter-Glo luminescent cell viability assay
    [PMID: 34731767]
    T98G IC50
    5.7 x 105 nM
    Compound: Temozolamide
    Antiproliferative activity against human T98G cells after 5 days by MTT assay
    Antiproliferative activity against human T98G cells after 5 days by MTT assay
    [PMID: 22608389]
    T98G IC50
    879 μM
    Compound: Temozolomide
    Growth inhibition of human T98G cells after 72 hrs by MTT assay
    Growth inhibition of human T98G cells after 72 hrs by MTT assay
    [PMID: 22809560]
    U138-MG IC50
    26 μM
    Compound: Temozolomide
    Cytotoxicity against human U138MG cells incubated for 48 hrs by MTT assay
    Cytotoxicity against human U138MG cells incubated for 48 hrs by MTT assay
    [PMID: 23069682]
    U-251 IC50
    > 100 μM
    Compound: TMZ
    Antiproliferative activity against human U251 cells after 48 hrs by MTT assay
    Antiproliferative activity against human U251 cells after 48 hrs by MTT assay
    [PMID: 26651221]
    U-251 EC50
    > 200 μM
    Compound: TMZ
    Antiproliferative activity against human U251MG cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    Antiproliferative activity against human U251MG cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    [PMID: 31978780]
    U-251 IC50
    > 200 μM
    Compound: TMZ
    Inhibition of cell proliferation of human U251 cells assessed as cell viability after 72 hrs by sulforhodamine B assay
    Inhibition of cell proliferation of human U251 cells assessed as cell viability after 72 hrs by sulforhodamine B assay
    [PMID: 25442304]
    U-251 IC50
    > 250 μM
    Compound: 1, TMZ
    Cytotoxicity against human U251 cells after 5 days by MTT assay
    Cytotoxicity against human U251 cells after 5 days by MTT assay
    [PMID: 24900418]
    U-251 IC50
    > 30 μM
    Compound: TMZ
    Antiproliferative activity against human U-251 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human U-251 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 34656900]
    U-251 IC50
    12.74 μM
    Compound: TMZ
    Cytotoxicity against human U-251MG cells assessed as decrease in cell viability incubated for 6 days by alamar blue assay
    Cytotoxicity against human U-251MG cells assessed as decrease in cell viability incubated for 6 days by alamar blue assay
    [PMID: 34384944]
    U-251 IC50
    36.4 μM
    Compound: Temozolomide
    Cytotoxicity against human U251 cells incubated for 24 hrs by MTT assay
    Cytotoxicity against human U251 cells incubated for 24 hrs by MTT assay
    [PMID: 31891260]
    U-251 IC50
    36.4 μM
    Compound: TMZ
    Cytotoxicity against human U-251 cells by MTT assay
    Cytotoxicity against human U-251 cells by MTT assay
    [PMID: 33915258]
    U-251 IC50
    455 μM
    Compound: TMZ
    Cytotoxicity against human U251MG cells assessed as reduction in cell survival measured after 72 hrs by MTT assay
    Cytotoxicity against human U251MG cells assessed as reduction in cell survival measured after 72 hrs by MTT assay
    [PMID: 30975504]
    U-251 IC50
    6.426 μM
    Compound: TMZ
    Cytotoxicity against cold atmospheric plasma (CAP)-treated human U-251MG cells assessed as decrease in cell viability treated with CAP for 30 secs followed by incubated with compound for 6 days by alamar blue assay
    Cytotoxicity against cold atmospheric plasma (CAP)-treated human U-251MG cells assessed as decrease in cell viability treated with CAP for 30 secs followed by incubated with compound for 6 days by alamar blue assay
    [PMID: 34384944]
    U-251 IC50
    7.284 μM
    Compound: TMZ
    Cytotoxicity against cold atmospheric plasma (CAP)-treated human U-251MG cells assessed as decrease in cell viability treated with CAP for 15 secs followed by incubated with compound for 6 days by alamar blue assay
    Cytotoxicity against cold atmospheric plasma (CAP)-treated human U-251MG cells assessed as decrease in cell viability treated with CAP for 15 secs followed by incubated with compound for 6 days by alamar blue assay
    [PMID: 34384944]
    U-373MG ATCC IC50
    220 μM
    Compound: Temozolomide
    Growth inhibition of human U373 cells after 72 hrs by MTT assay
    Growth inhibition of human U373 cells after 72 hrs by MTT assay
    [PMID: 22809560]
    U-373MG ATCC GI50
    369 μM
    Compound: 1; TMZ
    Growth inhibition of MGMT-transfected human U373 cells expressing MGMT after 7 days by MTT assay
    Growth inhibition of MGMT-transfected human U373 cells expressing MGMT after 7 days by MTT assay
    [PMID: 30108945]
    U-373MG ATCC GI50
    395 μM
    Compound: 1; TMZ
    Growth inhibition of MGMT-transfected human U373 cells after 7 days by MTT assay
    Growth inhibition of MGMT-transfected human U373 cells after 7 days by MTT assay
    10.1039/C6MD00384B
    U-373MG ATCC GI50
    68 μM
    Compound: 1; TMZ
    Growth inhibition of vehicle-transfected human U373 cells after 7 days by MTT assay
    Growth inhibition of vehicle-transfected human U373 cells after 7 days by MTT assay
    [PMID: 30108945]
    U-373MG ATCC GI50
    72.9 μM
    Compound: 1; TMZ
    Growth inhibition of empty vector transfected human U373 cells after 7 days by MTT assay
    Growth inhibition of empty vector transfected human U373 cells after 7 days by MTT assay
    10.1039/C6MD00384B
    U-87MG ATCC IC50
    > 200 μM
    Compound: TMZ
    Cytotoxicity against human U-87 MG cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
    Cytotoxicity against human U-87 MG cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
    [PMID: 34534673]
    U-87MG ATCC EC50
    > 200 μM
    Compound: TMZ
    Antiproliferative activity against human U87MG cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    Antiproliferative activity against human U87MG cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    [PMID: 31978780]
    U-87MG ATCC IC50
    > 200 μM
    Compound: TMZ
    Inhibition of cell proliferation of human U87MG cells assessed as cell viability after 72 hrs by sulforhodamine B assay
    Inhibition of cell proliferation of human U87MG cells assessed as cell viability after 72 hrs by sulforhodamine B assay
    [PMID: 25442304]
    U-87MG ATCC IC50
    > 30 μM
    Compound: TMZ
    Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 34656900]
    U-87MG ATCC IC50
    > 50 μM
    Compound: Temozolomide
    Cytotoxicity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 29789258]
    U-87MG ATCC IC50
    1.1 mM
    Compound: Temozolomide
    Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs under hypoxia condition by MTT assay
    Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs under hypoxia condition by MTT assay
    [PMID: 32186874]
    U-87MG ATCC IC50
    19.38 μM
    Compound: Temozolomide
    Cytotoxicity against human U87 cells assessed as growth inhibition after 72 hrs by SRB assay
    Cytotoxicity against human U87 cells assessed as growth inhibition after 72 hrs by SRB assay
    10.1039/C4MD00264D
    U-87MG ATCC IC50
    2898 μM
    Compound: TMZ
    Cytotoxicity against human U-87 MG cells using best fit nonlinear regression analysis
    Cytotoxicity against human U-87 MG cells using best fit nonlinear regression analysis
    [PMID: 35044783]
    U-87MG ATCC IC50
    3186 μM
    Compound: TMZ
    Cytotoxicity against human U-87 MG cells assessed as cell viability using raw interpretation method
    Cytotoxicity against human U-87 MG cells assessed as cell viability using raw interpretation method
    [PMID: 35044783]
    U-87MG ATCC IC50
    4.9 x 104 nM
    Compound: Temozolamide
    Antiproliferative activity against human U87 cells after 5 days by MTT assay
    Antiproliferative activity against human U87 cells after 5 days by MTT assay
    [PMID: 22608389]
    U-87MG ATCC IC50
    6.4 x 105 nM
    Compound: Temozolomide
    Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs under normoxia condition by MTT assay
    Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs under normoxia condition by MTT assay
    [PMID: 32186874]
    WiDr IC50
    1720 μM
    Compound: temozolomide
    Cytotoxicity against human WiDr cells overexpressing MGMT after 48 hrs by trypan blue staining-based hemocytometric analysis
    Cytotoxicity against human WiDr cells overexpressing MGMT after 48 hrs by trypan blue staining-based hemocytometric analysis
    [PMID: 25874335]
    WM 266-4 IC50
    > 100 μM
    Compound: TMZ
    Cytotoxicity against human WM 266-4 cells assessed as cell viability measured after 96 hrs by XTT assay
    Cytotoxicity against human WM 266-4 cells assessed as cell viability measured after 96 hrs by XTT assay
    [PMID: 34507011]
    體外研究
    (In Vitro)

    Temozolomide (TZM) 是一種甲基化劑,可穿過血腦屏障,適用于惡性神經(jīng)膠質瘤和轉移性黑色素瘤。Temozolomide 可有效對抗以低水平 O6-烷基鳥嘌呤 DNA 烷基轉移酶 (OGAT) 和功能錯配修復系統(tǒng) (MR)[1]為特征的腫瘤細胞。測定 Temozolomide (TZM) 在不同細胞系中的 IC50 值范圍為 14.1 至 234.6 μM,分為兩個明顯不同的組:低 IC50 的細胞系值 (<50 μM),包括 A172 (14.1±1.1 μM) 和 LN229 細胞 (14.5±1.1 μM),以及具有高 IC50 值 (>100 μM) 的那些,包括 SF268 (147.2±2.1 μM) 和 SK-N-SH 細胞 (234.6±2.3 μM)[3]。

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

    體內(nèi)研究
    (In Vivo)

    與對照相比,Temozolomide (TZM) 作為單一藥物不會顯著增加中值生存時間 (MST)。值得注意的是,在施用 100 或 200 mg/kg Temozolomide 之前,顱內(nèi)注射 NU1025 可顯著延長對照組或僅接受 Temozolomide 處理組的壽命。分割 Temozolomide 時,使用該方案獲得的壽命延長 (ILS) 高于 NU1025 聯(lián)合單次注射 Temozolomide 時觀察到的 (生存曲線統(tǒng)計比較:NU1025 顱內(nèi)注射 + Temozolomide 100 mg/kg×2 vs NU1025 + Temozolomide 200 mg/kg;P=0.023)[1]。

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

    Clinical Trial
    分子量

    194.15

    Formula

    C6H6N6O2

    CAS 號
    性狀

    固體

    顏色

    White to pink

    中文名稱

    替莫唑胺

    運輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式

    -20°C, protect from light, stored under nitrogen

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

    溶解性數(shù)據(jù)
    細胞實驗: 

    DMSO 中的溶解度 : 20.83 mg/mL (107.29 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)

    H2O 中的溶解度 : 2.86 mg/mL (14.73 mM; 超聲助溶)

    配制儲備液
    濃度 溶劑體積 質量 1 mg 5 mg 10 mg
    1 mM 5.1507 mL 25.7533 mL 51.5066 mL
    5 mM 1.0301 mL 5.1507 mL 10.3013 mL
    查看完整儲備液配制表

    * 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備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

    * 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質量
    =
    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

    動物實驗:

    請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實驗結果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用;
    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: ≥ 1.25 mg/mL (6.44 mM); 澄清溶液

      此方案可獲得 ≥ 1.25 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 12.5 mg/mL 的澄清 DMSO 儲備液加到 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: ≥ 1.25 mg/mL (6.44 mM); 澄清溶液

      此方案可獲得 ≥ 1.25 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 12.5 mg/mL 的澄清 DMSO 儲備液加到 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: PBS

      Solubility: 9.09 mg/mL (46.82 mM); 澄清溶液; 超聲助溶 (<60°C)

    動物溶解方案計算器
    請輸入動物實驗的基本信息:

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    由于實驗過程有損耗,建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動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。
    計算結果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。

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

    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,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,請謹慎選擇該方案。
    請確保第一步儲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: 99.98%

    參考文獻
    Cell Assay
    [1]

    The murine lymphoma cell line L5178Y of DBA/2 (H-2d/H-2d) origin is cultured in RPMI-1640 containing 10% fetal calf serum and antibiotics. Inhibition of PARP is obtained by treating cells (105 cells/mL) with 8-hydroxy-2-methylquinazolin-4[3H]-1 (NU1025), at a concentration (25 μM) that abrogates PARP activity. Cells are then exposed to Temozolomide (7.5-125 μM) and are cultured for 3 days. Cell growth is evaluated by counting viable cells in quadruplicate, and apoptosis is assessed by flow cytometry analysis of DNA content. Long-term survival is analyzed by colony-formation assay[1].

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

    Animal Administration
    [1]

    Mice[1]
    Male B6D2F1 (C57BL/6×DBA/2) mice are used. L5178Y cells (104 in 0.03 mL RPMI-1640) are then injected intracranially, through the center-middle area of the frontal bone to a 2-mm depth, using a 0.1-mL glass microsyringe and a 27-gauge disposable needle. To evaluate tumor cell growth, brains are fixed in 10% phosphate-buffered formaldehyde, and histologic sections (5 μm) are cut along the axial plane, stained with hematoxylin-eosin, and analyzed by light microscopy. Temozolomide is dissolved in DMSO (40 mg/mL), diluted in saline (5 mg/mL), and administered intraperitoneally on day 2 after tumor injection at 100 mg/kg or 200 mg/kg, doses commonly used for in vivo preclinical studies. Because cytotoxicity induced by Temozolomide and PARP inhibitors can be improved by fractionated modality of treatment, in selected groups a total dose of 200 mg/kg Temozolomide is divided in 2 doses of 100 mg/kg given on days 2 and 3.

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

    參考文獻

    完整儲備液配制表

    * 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備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 5.1507 mL 25.7533 mL 51.5066 mL 128.7664 mL
    5 mM 1.0301 mL 5.1507 mL 10.3013 mL 25.7533 mL
    10 mM 0.5151 mL 2.5753 mL 5.1507 mL 12.8766 mL
    DMSO 15 mM 0.3434 mL 1.7169 mL 3.4338 mL 8.5844 mL
    20 mM 0.2575 mL 1.2877 mL 2.5753 mL 6.4383 mL
    25 mM 0.2060 mL 1.0301 mL 2.0603 mL 5.1507 mL
    30 mM 0.1717 mL 0.8584 mL 1.7169 mL 4.2922 mL
    40 mM 0.1288 mL 0.6438 mL 1.2877 mL 3.2192 mL
    50 mM 0.1030 mL 0.5151 mL 1.0301 mL 2.5753 mL
    60 mM 0.0858 mL 0.4292 mL 0.8584 mL 2.1461 mL
    80 mM 0.0644 mL 0.3219 mL 0.6438 mL 1.6096 mL
    100 mM 0.0515 mL 0.2575 mL 0.5151 mL 1.2877 mL

    * 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

    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:
    Temozolomide
    目錄號:
    HY-17364
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