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  1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. Tanshinone IIA

Tanshinone IIA  (Synonyms: 丹參酮IIA; Dan Shen ketone)

目錄號: HY-N0135 純度: 99.78%
COA 產(chǎn)品使用指南

Tanshinone IIA (Tan IIA) 是丹參根中的主要組合物之一。Tanshinone IIA 可以通過靶向 VEGF/VEGFR2 的蛋白激酶結(jié)構(gòu)域來抑制血管生成。

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Tanshinone IIA Chemical Structure

Tanshinone IIA Chemical Structure

CAS No. : 568-72-9

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Customer Review

Other Forms of Tanshinone IIA:

    Tanshinone IIA purchased from MCE. Usage Cited in: J Transl Med. 2023 Jan 20;21(1):34.  [Abstract]

    Tanshinone IIA (Tan IIA; 24?h) significantly decreases the cell viability when concentration reaches to 50?μM in bEnd0.3 cells.

    Tanshinone IIA purchased from MCE. Usage Cited in: Eur J Pharmacol. 2020 Aug 5;880:173140.  [Abstract]

    Phospho-p65 (p-p65), p65, IL-1β, IL-6, TNF-α, and KLF4 expression in unligated, ligated and ligated + Tan IIA-treated carotid arteries is determined by Western blotting days 21 after carotid artery ligation.

    Tanshinone IIA purchased from MCE. Usage Cited in: J Pharm Pharmacol. 2018 Oct;70(10):1369-1377.  [Abstract]

    Tanshinone IIA induces TOV-21G apoptosis. Western blotting is performed with anti-Cleaved caspase 3 or anti-cleaved poly ADP-ribose polymerase (PARP) antibodies. Tubulin is loaded as the loading control.

    查看 VEGFR 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Tanshinone IIA (Tan IIA) is one of the main compositions in the root of Salvia miltiorrhiza Bunge. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2.

    IC50 & Target

    VEGF/VEGFR2[1]

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    2.2 μM
    Compound: 2a
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 34333396]
    A549 IC50
    53.2 μM
    Compound: Tan-IIA
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    [PMID: 30398868]
    A549 IC50
    6.68 μM
    Compound: 7; TSA
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by cell titer glo luminescent assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by cell titer glo luminescent assay
    [PMID: 35640078]
    AGS IC50
    10 μM
    Compound: 7, tanshinone iia
    Viability of human AGS cells under normoxic conditions after 24 hrs by MTT assay
    Viability of human AGS cells under normoxic conditions after 24 hrs by MTT assay
    [PMID: 17583950]
    AGS IC50
    6.8 μM
    Compound: 7, tanshinone iia
    Viability of human AGS cells under hypoxic conditions after 24 hrs by MTT assay
    Viability of human AGS cells under hypoxic conditions after 24 hrs by MTT assay
    [PMID: 17583950]
    AGS IC50
    7.53 μM
    Compound: 7, tanshinone iia
    Inhibition of HIF1 activation in human AGS cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay
    Inhibition of HIF1 activation in human AGS cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay
    [PMID: 17583950]
    BGC-823 IC50
    2.8 μM
    Compound: 10
    Anticancer activity against human BGC-823 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
    Anticancer activity against human BGC-823 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
    [PMID: 36332549]
    CWR22R IC50
    6.7 μM
    Compound: TS-IIA
    Cytotoxicity against human 22Rv1 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human 22Rv1 cells incubated for 72 hrs by MTT assay
    [PMID: 22175694]
    HeLa IC50
    193.2 μM
    Compound: Tan-IIA
    Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
    Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
    [PMID: 30398868]
    HeLa IC50
    3.47 μM
    Compound: 2a
    Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 34333396]
    Hep 3B2 IC50
    > 50 μM
    Compound: 7, tanshinone iia
    Viability of human Hep3B cells under normoxic conditions after 24 hrs by MTT assay
    Viability of human Hep3B cells under normoxic conditions after 24 hrs by MTT assay
    [PMID: 17583950]
    Hep 3B2 IC50
    > 50 μM
    Compound: 7, tanshinone iia
    Viability of human Hep3B cells under hypoxic conditions after 24 hrs by MTT assay
    Viability of human Hep3B cells under hypoxic conditions after 24 hrs by MTT assay
    [PMID: 17583950]
    Hep 3B2 IC50
    6.18 μM
    Compound: 7, tanshinone iia
    Inhibition of HIF1 activation in human Hep3B cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay
    Inhibition of HIF1 activation in human Hep3B cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay
    [PMID: 17583950]
    HepG2 IC50
    23.85 μM
    Compound: TSA
    Antiproliferative activity against human HepG2 cells by MTT assay
    Antiproliferative activity against human HepG2 cells by MTT assay
    [PMID: 33601313]
    HepG2 IC50
    4.91 μM
    Compound: 2a
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 34333396]
    HepG2 IC50
    65.7 μM
    Compound: Tan-IIA
    Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
    [PMID: 30398868]
    L02 IC50
    65.29 μM
    Compound: TSA
    Antiproliferative activity against human L02 cells by MTT assay
    Antiproliferative activity against human L02 cells by MTT assay
    [PMID: 33601313]
    L02 IC50
    78.5 μM
    Compound: Tan-IIA
    Antiproliferative activity against human L02 cells after 72 hrs by MTT assay
    Antiproliferative activity against human L02 cells after 72 hrs by MTT assay
    [PMID: 30398868]
    LNCaP IC50
    0.5 μM
    Compound: TS-IIA
    Cytotoxicity against human LNCAP cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human LNCAP cells incubated for 72 hrs by MTT assay
    [PMID: 22175694]
    LNCaP C4-2B IC50
    0.4 μM
    Compound: TS-IIA
    Cytotoxicity against human C4-2B cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human C4-2B cells incubated for 72 hrs by MTT assay
    [PMID: 22175694]
    MCF7 IC50
    > 5 μM
    Compound: 2a
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 34333396]
    MCF7 EC50
    0.9 μM
    Compound: Tan II-A
    Cytotoxicity against telomerase positive human MCF7 cells after 96 hrs by SRB assay
    Cytotoxicity against telomerase positive human MCF7 cells after 96 hrs by SRB assay
    [PMID: 22044621]
    MCF7 IC50
    7.7935 μM
    Compound: 2
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    [PMID: 33751939]
    MDA-MB-231 IC50
    115.9 μM
    Compound: Tan-IIA
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
    [PMID: 30398868]
    MDA-MB-231 IC50
    7.695 μM
    Compound: 2
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    [PMID: 33751939]
    MGC-803 IC50
    > 5 μM
    Compound: 2a
    Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 34333396]
    MIA PaCa-2 IC50
    1.9 μM
    Compound: 13
    Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay
    Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay
    [PMID: 21775156]
    NCI-N87 IC50
    3.1 μM
    Compound: 10
    Anticancer activity against human NCI-N87 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
    Anticancer activity against human NCI-N87 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
    [PMID: 36332549]
    PC-3 EC50
    1.2 μM
    Compound: Tan II-A
    Cytotoxicity against telomerase positive human PC3 cells after 96 hrs by SRB assay
    Cytotoxicity against telomerase positive human PC3 cells after 96 hrs by SRB assay
    [PMID: 22044621]
    PC-3 IC50
    3.3 μM
    Compound: TS-IIA
    Cytotoxicity against human PC3 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human PC3 cells incubated for 72 hrs by MTT assay
    [PMID: 22175694]
    SAOS-2 EC50
    > 20 μM
    Compound: Tan II-A
    Cytotoxicity against telomerase negative human Saos2 cells after 96 hrs by SRB assay
    Cytotoxicity against telomerase negative human Saos2 cells after 96 hrs by SRB assay
    [PMID: 22044621]
    SGC-7901 IC50
    250 μM
    Compound: 10
    Anticancer activity against human SGC-7901 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
    Anticancer activity against human SGC-7901 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
    [PMID: 36332549]
    U-937 IC50
    > 5 μM
    Compound: 2a
    Antiproliferative activity against human U-937 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Antiproliferative activity against human U-937 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 34333396]
    體外研究
    (In Vitro)

    Tanshinone IIA 的抗腫瘤作用包括抑制腫瘤細(xì)胞增殖、擾亂腫瘤細(xì)胞周期、促進(jìn)腫瘤細(xì)胞凋亡、抑制腫瘤細(xì)胞侵襲轉(zhuǎn)移等。Tanshinone IIA 對 A549 細(xì)胞具有抗增殖作用:24、48 和 72 h后 Tanshinone IIA 的 IC50 分別為 145.3、30.95 和 11.49 μM。CCK-8 測定用于評估分別用 Tanshinone IIA (2.5 -80 μM) 處理 24、48 和 72 小時的 A549 細(xì)胞的增殖活性。CCK-8 結(jié)果顯示 Tanshinone IIA 能以劑量和時間依賴性方式顯著抑制 A549 細(xì)胞增殖。藥物處理 48 小時后觀察到明顯的 A549 細(xì)胞凋亡和細(xì)胞生長抑制 (使用的濃度約為 IC50 值:Tanshinone IIA 31 μM 對 A549)。Western blotting 發(fā)現(xiàn),在 A549 細(xì)胞中暴露于 Tanshinone IIA (31 μM) 48 小時后,與載體相比,兩個藥物處理組的 VEGFVEGFR2 蛋白表達(dá)均下調(diào)[1]。
    Tanshinone IIA 是 Salvia miltiorrhiza 根中最豐富的成分之一,可保護(hù)大鼠心肌來源的 H9C2 細(xì)胞免于凋亡。用 Tanshinone IIA 處理 H9C2 細(xì)胞可通過下調(diào) PTEN (磷酸酶和張力蛋白同系物) 的表達(dá)來抑制血管緊張素 II 誘導(dǎo)的細(xì)胞凋亡,PTEN 是一種在細(xì)胞凋亡中起關(guān)鍵作用的腫瘤抑制因子。Tanshinone IIA 通過下調(diào)磷酸酶和張力蛋白同系物 (PTEN) 的表達(dá)來抑制血管緊張素 II (AngII) 誘導(dǎo)的細(xì)胞凋亡[2]。
    Tanshinone IIA 降低胃癌 AGS 細(xì)胞 EGFR 和 IGFR 蛋白表達(dá),阻斷 PI3K/Akt/mTOR 通路[3]。

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

    體內(nèi)研究
    (In Vivo)

    Tanshinone IIA (10 或 20 mg/kg;口服) 顯著逆轉(zhuǎn)東莨菪堿誘導(dǎo)的認(rèn)知障礙[1]。
    Tanshinone IIA (2、4、8 mg/kg;腹腔注射) 介導(dǎo)的保護(hù)作用對 STZ 誘導(dǎo)的糖尿病腎病的影響可能與通過減弱 PERK 信號活動減少內(nèi)質(zhì)網(wǎng)應(yīng)激有關(guān)[2]。
    Tanshinone IIA (3 和 12 mg/kg;ip) 顯著抑制異位子宮內(nèi)膜的生長[3]
    Tanshinone IIA 在一些研究中與 Tanshinone IIA sulfonate sodium (HY-N1370) 被互相替代使用,但存在水溶性、化學(xué)結(jié)構(gòu)、藥理活性和藥代動力學(xué)差異。動物給藥時請配置固體分散劑,或選擇使用水溶性較好的磺酸鹽形式 Tanshinone IIA sulfonate sodium (HY-N1370)[4]。

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

    Animal Model: Male ICR mice (25–30 g)[4]
    Dosage: 10 or 20 mg/kg
    Administration: P.o.
    Result: Significantly reversed scopolamine-induced cognitive impairments.
    Animal Model: STZ-treated rats[5]
    Dosage: 2, 4, 8 mg/kg
    Administration: I.p.
    Result: Decreased the expression levels of transforming growth factor-beta1, TSP-1, Grp78 and CHOP and attenuated the increase in the protein levels of p-PERK, p-elf2α and ATF-4 from the renal tissues of diabetic rats.
    Animal Model: Female Sprague-Dawley rats (180 -200g)[6]
    Dosage: 3 and 12 mg/kg
    Administration: I.p.
    Result: Significantly inhibited the growth of ectopic endometrium.
    分子量

    294.34

    Formula

    C19H18O3

    CAS 號
    性狀

    固體

    顏色

    Pink to red

    中文名稱

    丹參酮 IIA

    結(jié)構(gòu)分類
    初始來源
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    Powder -20°C 3 years
    4°C 2 years

    *該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。

    溶解性數(shù)據(jù)
    細(xì)胞實驗: 

    DMSO 中的溶解度 : 1 mg/mL (3.40 mM; 超聲助溶 (<80°C); 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)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 3.3974 mL 16.9872 mL 33.9743 mL
    5 mM --- --- ---
    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;該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。

    • 摩爾計算器

    • 稀釋計算器

    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

    動物實驗:

    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: 0.5% CMC-Na/0.1% Tween-80 in Saline water

      Solubility: 1 mg/mL (3.40 mM); 懸濁液; 超聲助溶

    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
    計算結(jié)果
    工作液所需濃度 : mg/mL
    純度 & 產(chǎn)品資料

    純度: 99.78%

    參考文獻(xiàn)

    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;該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3974 mL 16.9872 mL 33.9743 mL 84.9358 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:
    Tanshinone IIA
    目錄號:
    HY-N0135
    需求量: