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  1. Stem Cell/Wnt Apoptosis Autophagy
  2. Wnt β-catenin Apoptosis Autophagy
  3. Triptonide

Triptonide  (Synonyms: 雷公藤內(nèi)酯酮; NSC 165677; PG 492)

目錄號(hào): HY-32736 純度: 99.87%
COA 產(chǎn)品使用指南 技術(shù)支持

Triptonide (NSC 165677) 是從雷公藤中鑒定出的一種天然產(chǎn)物。Triptonide 是一種 Wnt 信號(hào)抑制劑,其 IC50 約為 0.3 nM。Triptonide 具有免疫抑制、抗炎、避育、神經(jīng)保護(hù)和抗淋巴瘤作用。

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

Triptonide Chemical Structure

Triptonide Chemical Structure

CAS No. : 38647-11-9

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10 mM * 1 mL in DMSO ¥1008
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10 mg ¥2046
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50 mg ¥5213
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Other Forms of Triptonide:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Triptonide (NSC 165677) is a natural product identified in Tripterygium wilfordii Hook F.. Triptonide is a Wnt signaling inhibitor with an IC50 of appropriately 0.3?nM. Triptonide has immunosuppression, anti-inflammatory, anti-fertility, neuroprotective and anti-lymphoma effects[1][2].

IC50 & Target

IC50: 0.3?nM (Wnt)[1]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
AGS IC50
< 20 nM
Compound: 8b
Cytotoxicity against human AGS cells incubated for 72 hrs by Alamar Blue method
Cytotoxicity against human AGS cells incubated for 72 hrs by Alamar Blue method
[PMID: 33289552]
ASPC1 IC50
< 20 nM
Compound: 8b
Antiproliferative activity against human ASPC1 incubated for 72 hrs by alamar blue assay
Antiproliferative activity against human ASPC1 incubated for 72 hrs by alamar blue assay
[PMID: 33289552]
BXPC-3 IC50
< 20 nM
Compound: 8b
Antiproliferative activity against human BXPC-3 incubated for 72 hrs by alamar blue assay
Antiproliferative activity against human BXPC-3 incubated for 72 hrs by alamar blue assay
[PMID: 33289552]
CFPAC-1 IC50
< 20 nM
Compound: 8b
Antiproliferative activity against human CFPAC-1 incubated for 72 hrs by alamar blue assay
Antiproliferative activity against human CFPAC-1 incubated for 72 hrs by alamar blue assay
[PMID: 33289552]
DU-145 IC50
0.01 μM
Compound: 8b
Antiproliferative activity against human DU-145 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human DU-145 cells incubated for 72 hrs by CCK8 assay
[PMID: 33289552]
HGC-27 IC50
< 20 nM
Compound: 8b
Cytotoxicity against human HGC-27 cells incubated for 72 hrs by Alamar Blue method
Cytotoxicity against human HGC-27 cells incubated for 72 hrs by Alamar Blue method
[PMID: 33289552]
Jurkat IC50
4 nM
Compound: 8b
Antiproliferative activity against human Jurkat cells incubated for 3 to 6 days by alamar blue assay
Antiproliferative activity against human Jurkat cells incubated for 3 to 6 days by alamar blue assay
[PMID: 33289552]
LNCaP IC50
10 nM
Compound: 8b
Antiproliferative activity against human LNCaP cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human LNCaP cells incubated for 72 hrs by CCK8 assay
[PMID: 33289552]
MCF7 IC50
0.03 μM
Compound: Triptonide
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 28759877]
MDA-MB-231 IC50
0.03 μM
Compound: Triptonide
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 28759877]
MGC-803 IC50
< 20 nM
Compound: 8b
Cytotoxicity against human MGC-803 cells incubated for 72 hrs by Alamar Blue method
Cytotoxicity against human MGC-803 cells incubated for 72 hrs by Alamar Blue method
[PMID: 33289552]
NCI-N87 IC50
< 20 nM
Compound: 8b
Cytotoxicity against human NCI-N87 cells incubated for 72 hrs by Alamar Blue method
Cytotoxicity against human NCI-N87 cells incubated for 72 hrs by Alamar Blue method
[PMID: 33289552]
PANC-1 IC50
< 20 nM
Compound: 8b
Cytotoxicity against human Panc-1 cells incubated for 72 hrs by alamar blue assay
Cytotoxicity against human Panc-1 cells incubated for 72 hrs by alamar blue assay
[PMID: 33289552]
PANC-1 IC50
47 nM
Compound: Triptonide
Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability after 72 hrs
Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability after 72 hrs
[PMID: 31889668]
PC-3 IC50
0.012 μM
Compound: 8b
Antiproliferative activity against human PC-3 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human PC-3 cells incubated for 72 hrs by CCK8 assay
[PMID: 33289552]
PC-3 IC50
0.02 μM
Compound: Triptonide
Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 28759877]
PC-3 IC50
0.026 μM
Compound: 2
Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation by sulforhodamine B assay
Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation by sulforhodamine B assay
[PMID: 25467158]
PC-3 IC50
0.6 μM
Compound: 2
Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay
Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay
[PMID: 20833543]
PC-3 IC50
25 nM
Compound: Triptonide
Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31889668]
Raji IC50
4 nM
Compound: 8b
Antiproliferative activity against human Raji cells incubated for 3 to 6 days by alamar blue assay
Antiproliferative activity against human Raji cells incubated for 3 to 6 days by alamar blue assay
[PMID: 33289552]
RKO IC50
15 nM
Compound: 8b
Cytotoxicity against human RKO cells incubated for 72 hrs by Cell Titer-Glo luminescence assay
Cytotoxicity against human RKO cells incubated for 72 hrs by Cell Titer-Glo luminescence assay
[PMID: 33289552]
SGC-7901 IC50
< 20 nM
Compound: 8b
Cytotoxicity against human SGC-7901 cells incubated for 72 hrs by Alamar Blue method
Cytotoxicity against human SGC-7901 cells incubated for 72 hrs by Alamar Blue method
[PMID: 33289552]
SK-OV-3 IC50
0.008 μM
Compound: Triptonide
Cytotoxicity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 28759877]
SK-OV-3 IC50
0.008 μM
Compound: 2
Antiproliferative activity against human SKOV3 cells after 72 hrs by SRB assay
Antiproliferative activity against human SKOV3 cells after 72 hrs by SRB assay
[PMID: 20833543]
SW1990 IC50
< 20 nM
Compound: 8b
Antiproliferative activity against human SW1990 incubated for 72 hrs by alamar blue assay
Antiproliferative activity against human SW1990 incubated for 72 hrs by alamar blue assay
[PMID: 33289552]
SW480 IC50
17 nM
Compound: 8b
Cytotoxicity against human SW480 cells incubated for 72 hrs by Cell Titer-Glo luminescence assay
Cytotoxicity against human SW480 cells incubated for 72 hrs by Cell Titer-Glo luminescence assay
[PMID: 33289552]
U-251 IC50
0.031 μM
Compound: 2
Cytotoxicity against human U251 cells assessed as inhibition of cell proliferation by sulforhodamine B assay
Cytotoxicity against human U251 cells assessed as inhibition of cell proliferation by sulforhodamine B assay
[PMID: 25467158]
體外研究
(In Vitro)

Triptonide 通過 β-catenin 的 C 末端反式激活結(jié)構(gòu)域阻斷 Wnt/β-catenin 信號(hào)通路,促進(jìn) Wnt 依賴性癌細(xì)胞的凋亡[1]
Triptonide 有效抑制人癌細(xì)胞的增殖 B 淋巴瘤 Raji 和 T 淋巴瘤 Jurkat 細(xì)胞的 IC50 分別為 5.7 nM 和 4.8 nM[2]。
Triptonide (2.5-10 nM;6 天) 顯著抑制 B 淋巴瘤細(xì)胞集落形成能力[2]
Triptonide (20 nM;3 天) 通過激活 PARP 和半胱天冬酶 3 促進(jìn)細(xì)胞凋亡,但減少 BCL2淋巴瘤細(xì)胞中的蛋白質(zhì)水平[2]。
Triptonide (5-10 nM;72 小時(shí)) 顯著降低 Lyn 總蛋白和磷酸化蛋白,并減少 Lyn 下游 ERK 和 ATK 信號(hào)通路[2]。

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

Cell Proliferation Assay[2]

Cell Line: B-lymphoma Raji cells, T-lymphoma Jurkat cells
Concentration: 0-80 nM
Incubation Time: 3 days, 6 days
Result: Inhibited lymphoma cell tumorigenic capability in a dose-dependent manner.

Apoptosis Analysis[2]

Cell Line: Raji cells
Concentration: 5 nM, 10 nM, 20 nM
Incubation Time: 3 days
Result: Did not significantly induce apoptosis at the effective tumor growth-inhibitory (2.5-10 nM); moderately induced lymphoma cell apoptosis (20 nM).

Western Blot Analysis[2]

Cell Line: Raji cells
Concentration: 5 nM, 10 nM, 20 nM
Incubation Time: 3 days
Result: Did not vigorously activated pro-apoptotic proteins PARP and caspase 3 in lymphoma cells (5-10 nM); significantly activated PARP and caspase 3 (20 nM); significantly reduced anti-apoptotic BCL2 levels.

RT-PCR[2]

Cell Line: Raji cells
Concentration: 5 nM, 10 nM
Incubation Time: 72 hours
Result: Significantly diminished Lyn mRNA levels in the lymphoma cells.
體內(nèi)研究
(In Vivo)

Triptonide (5 mg/kg;腹腔注射;每天;持續(xù) 34 天) 對(duì)小鼠具有很強(qiáng)的抗淋巴瘤作用[2]。

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

Animal Model: Eight-week-old female NOD/SCID mice (18-22 g), with 3 x 107 Raji cells xenograft[2]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection, daily, for 34 days
Result: Potently inhibited lymphoma cell growth and tumorigenic capability.
分子量

358.39

Formula

C20H22O6

CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

雷公藤內(nèi)酯酮;雷藤酮;雷公藤羰內(nèi)酯

結(jié)構(gòu)分類
初始來源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 50 mg/mL (139.51 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.7903 mL 13.9513 mL 27.9026 mL
5 mM 0.5581 mL 2.7903 mL 5.5805 mL
查看完整儲(chǔ)備液配制表

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

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

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

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(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(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.98 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 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。
  • 方案 二

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.98 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,此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    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玉米油中,混合均勻。

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

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 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(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)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(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.89%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

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

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7903 mL 13.9513 mL 27.9026 mL 69.7564 mL
5 mM 0.5581 mL 2.7903 mL 5.5805 mL 13.9513 mL
10 mM 0.2790 mL 1.3951 mL 2.7903 mL 6.9756 mL
15 mM 0.1860 mL 0.9301 mL 1.8602 mL 4.6504 mL
20 mM 0.1395 mL 0.6976 mL 1.3951 mL 3.4878 mL
25 mM 0.1116 mL 0.5581 mL 1.1161 mL 2.7903 mL
30 mM 0.0930 mL 0.4650 mL 0.9301 mL 2.3252 mL
40 mM 0.0698 mL 0.3488 mL 0.6976 mL 1.7439 mL
50 mM 0.0558 mL 0.2790 mL 0.5581 mL 1.3951 mL
60 mM 0.0465 mL 0.2325 mL 0.4650 mL 1.1626 mL
80 mM 0.0349 mL 0.1744 mL 0.3488 mL 0.8720 mL
100 mM 0.0279 mL 0.1395 mL 0.2790 mL 0.6976 mL
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產(chǎn)品名稱:
Triptonide
目錄號(hào):
HY-32736
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