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  1. JAK/STAT Signaling Stem Cell/Wnt Autophagy
  2. STAT Autophagy
  3. Cryptotanshinone

Cryptotanshinone  (Synonyms: 隱丹參酮; Cryptotanshinon; Tanshinone c)

目錄號: HY-N0174 純度: 98.70%
COA 產(chǎn)品使用指南 技術(shù)支持

Cryptotanshinone是從丹參的根中提取的天然化合物,具有抗腫瘤活性。 Cryptotanshinone抑制 STAT3IC50 為4.6 μM。

MCE 的所有產(chǎn)品僅用作科學(xué)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(wù)

Cryptotanshinone Chemical Structure

Cryptotanshinone Chemical Structure

CAS No. : 35825-57-1

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10 mM * 1 mL in DMSO ¥355
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1 mg ¥109
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5 mg ¥218
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10 mg ¥350
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Customer Review

Other Forms of Cryptotanshinone:

MCE 顧客使用本產(chǎn)品發(fā)表的 37 篇科研文獻

IF
WB

    Cryptotanshinone purchased from MCE. Usage Cited in: Eur J Pharmacol. 2022 Nov 30;175434.  [Abstract]

    Cryptotanshinone (CTS; 0, 10, 20 μМ; 24 h) significantly decreases the expression of Col-I and (when at 20 μМ) Col-III, α-SMA, in WPMY-1 cells.

    Cryptotanshinone purchased from MCE. Usage Cited in: Eur J Pharmacol. 2022 Nov 30;175434.  [Abstract]

    Cryptotanshinone (CTS; 10, 20 μМ; 24 h) promotes apoptosis of BPH-1 (fig A) and WPMY-1 (fig B) cells.

    查看 STAT 亞型特異性產(chǎn)品:

    • 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

    Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.

    IC50 & Target[1]

    STAT3

    4.6 μM (IC50)

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    AGS IC50
    1.58 μM
    Compound: 3, cryptotanshinone
    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]
    AGS IC50
    10.2 μM
    Compound: 3, cryptotanshinone
    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
    13.5 μM
    Compound: 3, cryptotanshinone
    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]
    BaF3 IC50
    17.22 μM
    Compound: Cryptotanshinone
    Growth inhibition of IL3-stimulated mouse BA/F3 cells after 48 hrs by CellTiter 96 assay
    Growth inhibition of IL3-stimulated mouse BA/F3 cells after 48 hrs by CellTiter 96 assay
    [PMID: 23957426]
    ECa-109 cell line IC50
    5.01 μM
    Compound: 8
    Antitumor activity against human EC109 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antitumor activity against human EC109 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 35504209]
    HCT-116 IC50
    4.6 μM
    Compound: 47
    Inhibition of STAT3 expressed in human HCT116 cells after 24 hrs by luciferase reporter gene assay
    Inhibition of STAT3 expressed in human HCT116 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 22650325]
    Hep 3B2 IC50
    > 30 μM
    Compound: 3, cryptotanshinone
    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
    > 30 μM
    Compound: 3, cryptotanshinone
    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
    1.36 μM
    Compound: 3, cryptotanshinone
    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
    29.2 μM
    Compound: 8
    Antitumor activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antitumor activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 35504209]
    KB 3-1 IC50
    6.9 μM
    Compound: 1
    Cytotoxicity against drug-sensitive human KB-3-1 cells after 48 hrs by MTS/PMS assay
    Cytotoxicity against drug-sensitive human KB-3-1 cells after 48 hrs by MTS/PMS assay
    [PMID: 11720520]
    KB-V1 IC50
    7.5 μM
    Compound: 1
    Cytotoxicity against multidrug-resistant human KBV1 cells after 48 hrs by MTS/PMS assay
    Cytotoxicity against multidrug-resistant human KBV1 cells after 48 hrs by MTS/PMS assay
    [PMID: 11720520]
    MIA PaCa-2 IC50
    5.8 μM
    Compound: 14
    Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay
    Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay
    [PMID: 21775156]
    Vero C1008 CC50
    > 300 μM
    Compound: 28
    Cytotoxicity against African green monkey Vero E6 cells assessed as cell viability treated for 24 hrs by CCK8 assay
    Cytotoxicity against African green monkey Vero E6 cells assessed as cell viability treated for 24 hrs by CCK8 assay
    [PMID: 35620927]
    體外研究
    (In Vitro)

    Cryptotanshinone 顯著抑制 STAT3 依賴的熒光素酶活性、STAT3 Tyr705 磷酸化和 STAT3 二聚化,相比之下,Tanshinone IIA 不表現(xiàn)任何活性。Cryptotanshinone (7 μM) 顯著阻斷 DU145 細胞中 STAT3 Tyr705 磷酸化,但不影響 STAT3 Ser727 磷酸化,且以 IC50 約 5 μM 顯著抑制 JAK2 的磷酸化,而不影響上游激酶 c-Src 和 EGFR 的磷酸化,表明 STAT3 Tyr705 磷酸化的抑制可能通過直接機制實現(xiàn),可能是通過與 STAT3 的 SH2 結(jié)構(gòu)域結(jié)合。Cryptotanshinone 顯著抑制 DU145 前列腺癌細胞中具有活性 STAT3 的增殖,GI50 為 7 μM,作用機制是阻斷 STAT3 活性,導(dǎo)致 cyclin D1、Bcl-xL 和 survivin 的下調(diào),從而引起 G0-G1 期細胞累積。Cryptotanshinone 對 PC3、LNCaP 和 MDA-MB-468 細胞的增殖抑制作用較弱[1]。Cryptotanshinone 顯著減弱 DEX 對卵巢的激素效應(yīng),包括培養(yǎng)基中睪酮 (T) 的顯著降低及孕酮 (P) 的升高。Cryptotanshinone 顯著增加 DEX 處理的卵巢中 AKT2 和 GSK3β 的磷酸化水平[2]。Cryptotanshinone 和 Imatinib 聯(lián)合處理對 Imatinib 敏感和耐藥的慢性粒細胞白血病 (CML) 細胞系以及原代 CML 細胞表現(xiàn)出顯著的協(xié)同殺傷作用[3]。

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

    體內(nèi)研究
    (In Vivo)

    Cryptotanshinone 可逆轉(zhuǎn)卵巢 IR,并顯著增加接受 DEX 治療的小鼠所有檢查組織中的 2-脫氧-D-[1,2-3H]-葡萄糖攝取量。Cryptotanshinone 可顯著降低排卵率和血漿 E2 和 P 水平[2]。Cryptotanshinone 給藥可顯著降低 ob/ob 小鼠 (C57BL/6J-Lepob) 和飲食誘導(dǎo)肥胖 (DIO) 小鼠的體重和食物攝入量,且呈劑量依賴性。與對照組小鼠相比,Cryptotanshinone 可顯著減少脂肪組織中的脂肪,顯著降低血清甘油三酯和膽固醇水平,骨骼肌的 AMPK 活性提高 2.5 至 3 倍。以 600 mg/kg/天的劑量口服Cryptotanshinone 可顯著降低 ob/ob 小鼠 (C57BL/6J-Lepob)、db/db 小鼠 (C57BL/KsJ-Leprdb) 和 ZDF 大鼠的血糖水平,這種效果在 3 天后出現(xiàn),并持續(xù)整個監(jiān)測期[4]

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

    分子量

    296.36

    Formula

    C19H20O3

    CAS 號
    性狀

    固體

    顏色

    Pink to red

    中文名稱

    隱丹參酮;隱丹參醌;丹參酮 C

    結(jié)構(gòu)分類
    初始來源
    運輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    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)
    細胞實驗: 

    DMSO 中的溶解度 : 5 mg/mL (16.87 mM; 超聲助溶 (<60°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)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 3.3743 mL 16.8714 mL 33.7427 mL
    5 mM 0.6749 mL 3.3743 mL 6.7485 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(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時,請在1年內(nèi)使用, -20°C儲存時,請在6個月內(nèi)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:

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

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實驗的工作液,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: 0.83 mg/mL (2.80 mM); 懸濁液; 超聲助溶

      此方案可獲得 0.83 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 8.3 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: ≥ 0.83 mg/mL (2.80 mM); 澄清溶液

      此方案可獲得 ≥ 0.83 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 8.3 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: Corn Oil

      Solubility: 8 mg/mL (26.99 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
    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(jié)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)。
    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(shù)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: 98.70%

    參考文獻
    Kinase Assay
    [1]

    HCT-116 cells are transiently transfected with reporter plasmid having the STAT3-binding element for regulating luciferase assay. Cells are treated with Cryptotanshinone for 24 hours at a concentration range of 0.2 to 50 μM. After treatment, cells are harvested in 20 μL of passive lysis buffer and luciferase activity is evaluated by the Dual Luciferase Reporter Assay kit on Wallac Victor2. The concentration of Cryptotanshinone that inhibits the luciferase activity by 50% represents IC50 value.

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

    Cell Assay
    [3]

    The MTT assay is used for the assessment of cell growth inhibition as described previously. Cells are seeded at a density of 8000 cells per well in 96-well plates in RPMI-1640 containing 10% FBS. Different concentrations of imatinib and CPT are added and incubated for another 24 h. Then, 20 μL of MTT are added into each well and the absorbance at 570 nm is measured on an enzyme linked immunosorbent assay (ELISA) plate reader. The coefficient of drug interaction (CDI) between imatinib and CPT is determined according to a previous study. The calculated method is as follows: CDI/AB/(A × B). According to the absorbance of each group, AB is the ratio of the combination group to the control group; A or B is the ratio of the single agent group to the control group. CDI < 1 indicates a synergistic effect; CDI=1 indicates an additive effect; CDI > 1 indicates an antagonistic effect. In the combination treatment group, the concentrations of CPT are arbitrarily designated according to the 50% inhibitory concentration (IC50) value. Then, the cell viabilities are determined after treatment with different concentrations of imatinib plus CPT (constant CPT concentration for one cell type). Finally, the combination IC50 values of imatinib are calculated, and are represented in Table I. The primary CML cells CP1 to CP3 are isolated from patients in chronic phase, while BC1 and BC2 are isolated from patients in blast crisis. Three independent sets of experiments are performed. The IC50 values are presented as the mean±standard deviation (SD).

    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(fù)凍融造成的產(chǎn)品失效
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時,請在1年內(nèi)使用, -20°C儲存時,請在6個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3743 mL 16.8714 mL 33.7427 mL 84.3569 mL
    5 mM 0.6749 mL 3.3743 mL 6.7485 mL 16.8714 mL
    10 mM 0.3374 mL 1.6871 mL 3.3743 mL 8.4357 mL
    15 mM 0.2250 mL 1.1248 mL 2.2495 mL 5.6238 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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    產(chǎn)品名稱:
    Cryptotanshinone
    目錄號:
    HY-N0174
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