Triptolide

別名: PG490, NSC 163062 中文名稱：雷公藤甲素

目錄號：S3604 Purity: 99.95%

Triptolide是一種三環(huán)氧二萜類化合物,是從中草藥雷公藤中提取的免疫抑制劑。它是一種NF-κB抑制劑，抑制NF-κB轉(zhuǎn)錄活性，破壞p65/CBP的相互作用，減少p65蛋白。Triptolide (PG490) 可抑制 heat shock transcription factor 1 (HSF1) 的反式激活。Triptolide 可抑制 MDM2 并通過一個p53非依賴性通路來誘導凋亡。

Triptolide Chemical Structure

CAS: 38748-32-2

規(guī)格	價格	庫存
10mM (1mL in DMSO)	2432.43	現(xiàn)貨
1mg	576.89	現(xiàn)貨
5mg	2060.55	現(xiàn)貨
100mg	16298.78	現(xiàn)貨
1g	39900	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.95%

99.95

Triptolide相關(guān)產(chǎn)品

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相關(guān)化合物庫	FDA藥物庫免疫/炎癥分子化合物庫小分子免疫腫瘤化合物庫 NF-κB信號通路庫 FDA抗癌藥物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
Pkd1-/-	Increase in	100 nM	96 hrs	Increase in p21CIP/WAF expression in mouse Pkd1-/- cells at 100 nM after 96 hrs by Western blot analysis	17360534
Pkd2+/-	Growth inhibition of PC2 expressing mouse	100 nM	24 hrs	Growth inhibition of PC2 expressing mouse Pkd2+/- cells as cell death at 100 nM after 24 hrs	17360534
KBM5	Cytotoxicity against	0.001 to 17 uM	72 hrs	Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl at 0.001 to 17 uM after 72 hrs by MTS assay	20149665
KBM5	Cytotoxicity against	0.001 to 17 uM	72 hrs	Cytotoxicity against imatinib-resistant human KBM5 cells harboring Bcr-Abl T315I mutant at 0.001 to 17 uM after 72 hrs by MTS assay	20149665
LNCAP	Antagonist activity at	5 uM	24 hrs	Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced receptor transcriptional activity at 5 uM after 24 hrs by dual luciferase reporter gene assay	27994731
LNCAP	Antagonist activity at	500 nM	24 hrs	Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced receptor transcriptional activity at 500 nM after 24 hrs by dual luciferase reporter gene assay	27994731
HepG2	Antitumor activity against	0.2 mg/kg	15 days	Antitumor activity against human HepG2 cells xenografted in Balb/c nude mouse assessed as reduction in tumor growth at 0.2 mg/kg, ip administered once daily for 15 days	30613335
Pkd1+/-	Increase in	100 nM		Increase in PC2 dependent calcium release in mouse Pkd1+/- cells at 100 nM	17360534
Pkd1-/-	Increase in	100 nM		Increase in PC2 dependent calcium release in mouse Pkd1-/- cells at 100 nM	17360534
Pkd1-/-	Increase in	50 uM		Increase in calcium release in mouse Pkd1-/- cells at 50 uM in presence of RyR antagonist dantrolene	17360534
SMMC7721	Cytotoxicity against		72 hrs	Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay, IC50=0.018μM	19637874
A549	Cytotoxic activity against		72 hrs	Cytotoxic activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0175μM	28011223
MOLT4	Cytotoxicity against		72 hrs	Cytotoxicity against human MOLT4 cells after 72 hrs by MTT assay, IC50=0.017μM	19637874
SGC7901	Cytotoxicity against		72 hrs	Cytotoxicity against human SGC7901 cells after 72 hrs by MTT assay, IC50=0.015μM	19637874
Rh30	Cytotoxicity against		72 hrs	Cytotoxicity against human Rh30 cells after 72 hrs by MTT assay, IC50=0.014μM	19637874
KBM5	Cytotoxicity against		72 hrs	Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl after 72 hrs by MTS assay, IC50=0.0103μM	20149665
SKOV3	Cytotoxicity against		72 hrs	Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay, IC50=0.01μM	19637874
HCT116	Cytotoxicity against		72 hrs	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.01μM	19637874
KBM5	Cytotoxicity against		72 hrs	Cytotoxicity against imatinib-resistant human KBM5 cells harboring Bcr-Abl T315I mutant after 72 hrs by MTS assay, IC50=0.0083μM	20149665
SKOV3	Cytotoxic activity against		72 hrs	Cytotoxic activity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0072μM	28011223
SKOV3	Cytotoxicity against		72 hrs	Cytotoxicity against human SKOV3 cells after 72 hrs by sulforhodamine B assay, IC50=0.006μM	24378709
SKOV3	Antiproliferative activity against		72 hrs	Antiproliferative activity against human SKOV3 cells after 72 hrs by SRB assay, IC50=0.006μM	20833543
PC3	Cytotoxic activity against		72 hrs	Cytotoxic activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0183μM	28011223
MCF7	Cytotoxicity against		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50=0.019μM	19637874
Bel7402	Cytotoxicity against		72 hrs	Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay, IC50=0.02μM	19637874
PC3	Antiproliferative activity against		72 hrs	Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay, IC50=0.02μM	20833543
PC3	Cytotoxicity against		72 hrs	Cytotoxicity against human PC3 cells after 72 hrs by sulforhodamine B assay, IC50=0.02μM	24378709
786-O	Cytotoxicity against		72 hrs	Cytotoxicity against human 786-O cells after 72 hrs by MTT assay, IC50=0.022μM	19637874
MDA-MB-231	Cytotoxicity against		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=0.024μM	19637874
DU145	Cytotoxicity against		72 hrs	Cytotoxicity against human DU145 cells after 72 hrs by MTT assay, IC50=0.024μM	19637874
HO8910	Cytotoxicity against		72 hrs	Cytotoxicity against human HO8910 cells after 72 hrs by MTT assay, IC50=0.028μM	19637874
HCT15	Cytotoxicity against		72 hrs	Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay, IC50=0.029μM	19637874
32D	Cytotoxicity against		72 hrs	Cytotoxicity against mouse 32D cells harboring wild type Bcr-Abl after 72 hrs by MTS assay, IC50=0.032μM	20149665
32D	Cytotoxicity against		72 hrs	Cytotoxicity against imatinib-resistant mouse 32D cells harboring Bcr-Abl T315I mutant after 72 hrs by MTS assay, IC50=0.034μM	20149665
PC3	Cytotoxicity against		72 hrs	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50=0.043μM	19637874
KB	Cytotoxicity against		72 hrs	Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=0.043μM	19637874
HepG2	Cytotoxicity against		48 hrs	Cytotoxicity against human HepG2 cells after 48 hrs by XTT assay, IC50=0.0433μM	30613335
HeLa	Cytotoxicity against		72 hrs	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50=0.047μM	19637874
U251	Cytotoxicity against		72 hrs	Cytotoxicity against human U251 cells after 72 hrs by MTT assay, IC50=0.049μM	19637874
K562	Cytotoxicity against		72 hrs	Cytotoxicity against human K562 cells after 72 hrs by MTT assay, IC50=0.05μM	19637874
SW1116	Cytotoxicity against		72 hrs	Cytotoxicity against human SW1116 cells after 72 hrs by MTT assay, IC50=0.052μM	19637874
A549	Cytotoxicity against		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=0.059μM	19637874
MKN28	Cytotoxicity against		72 hrs	Cytotoxicity against human MKN28 cells after 72 hrs by MTT assay, IC50=0.2μM	19637874
A549	Antagonist activity at			Antagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assay, IC50=0.014μM	23895492
MDA-MB-468	Cytotoxicity against			Cytotoxicity against human MDA-MB-468 cells by SRB assay, IC50=0.01μM	19637874
SKOV3	Cytotoxicity against			Cytotoxicity against human SKOV3 cells by SRB assay, IC50=0.009μM	19637874
HCT116	Cytotoxicity against			Cytotoxicity against human HCT116 cells assessed as decrease in cell viability, IC50=0.0047μM	31121546
HT-29	Cytotoxicity against			Cytotoxicity against human HT-29 cells, IC50=0.0021μM	21470864
A549	Cytotoxicity against			Cytotoxicity against human A549 cells, IC50=0.019μM	21470864
PC3	Cytotoxicity against			Cytotoxicity against human PC3 cells by SRB assay, IC50=0.02μM	19637874
PC3	Cytotoxicity against			Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation by sulforhodamine B assay, IC50=0.02μM	25467158
A549	Antagonist activity at			Antagonist activity at human PAR2 expressed in human A549 cells coexpressing TACR1 assessed as inhibition of substance P-induced IL-8 production by ELISA, IC50=0.023μM	23895492
A549	Growth inhibition of human			Growth inhibition of human A549 cells, IC50=0.03μM	28814374
U251	Cytotoxicity against			Cytotoxicity against human U251 cells assessed as inhibition of cell proliferation by sulforhodamine B assay, IC50=0.033μM	25467158
NIH/3T3	Cytotoxicity against			Cytotoxicity against mouse NIH/3T3 cells assessed as decrease in cell viability, IC50=0.05μM	31121546
HeLa	Cytotoxicity against			Cytotoxicity against human HeLa cells assessed as decrease in cell viability, IC50=0.087μM	31121546
Jurkat	Cytotoxicity against			Cytotoxicity against human Jurkat cells assessed as decrease in cell viability, IC50=0.14μM	31121546
MDCK	Cytotoxicity against			Cytotoxicity against MDCK cells assessed as decrease in cell viability, IC50=1.2μM	31121546
Pkd1-/-	Induction of			Induction of cell growth arrest in mouse Pkd1-/- cells in presence of calcium	17360534
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生物活性

產(chǎn)品描述

靶點

NF-κB ^[1]

HSF1 ^[1]

MDM2 ^[1]

體外研究(In Vitro)
體外研究活性	Triptolide是一種三環(huán)氧二萜類化合物，具有強效的免疫抑制和抗炎性能。在嘌呤盒/核因子和NF-κB介導的轉(zhuǎn)錄激活水平，Triptolide能夠抑制激活的T細胞中IL-2的表達。^[1] Triptolide在極低濃度下(2–10納克/毫升)能夠抑制腫瘤細胞的增殖和集落形成。Triptolide對乳腺癌，胃癌和白血病細胞系HL-60細胞具有抑制活性。在腫瘤細胞中，Triptolide通過阻斷NF-κB激活并使腫瘤細胞對TNF-&alpha誘導的程序性細胞死亡敏感來誘導細胞凋亡。^[2]
實驗圖片	檢測方法	檢測指標	實驗圖片	PMID
	Western blot	c-Jun MDM2 p-AKT / AKT / p-Foxo3a / Foxo3a / p53 p-PI3K / PI3K / p85 / p110		22666381
	Growth inhibition assay	Cell viability		22666381

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	Triptolide與cyclosporin A協(xié)同促進動物模型中移植物的存活，并協(xié)同抑制同種異體骨髓移植伴隨的移植物抗宿主病。此外，通過抑制c-IAP2 和c-IAP1的誘導作用，它會引起腫瘤細胞的細胞凋亡，同時部分增強腫瘤壞死因子(TNF-α)誘導的細胞凋亡。^[1] ^[3] Triptolide治療2-3周抑制由四種不同腫瘤細胞系(B16 黑色素瘤，MDA-435 乳腺癌，TSU 膀胱癌，以及MGC80-3 胃癌)形成的異種移植物的生長，表明TPL具有廣譜的抗腫瘤活性，對野生型和突變體p53均具有作用。此外，在實驗中，Triptolide抑制B16F10細胞轉(zhuǎn)移到小鼠的肺和脾臟中。^[2] 在小鼠模型中，Triptolide在體內(nèi)外均具有抗多囊性腎病的作用。^[4] LD50: 小鼠0.83毫克/千克(靜脈注射)。 ^[5]

參考文獻
[1] Qiu D, et al. J Biol Chem, 1999, 274(19), 13443-13450. [2] Yang S, et al. Mol Cancer Ther, 2003, 2(1), 65-72. [3] Lee KY, et al. J Biol Chem, 1999, 274(19), 13451-13455. [4] Leuenroth SJ, et al. Proc Natl Acad Sci, 2007, 104(11), 4389-4394. [5] Xu L, et al. Food Chem Toxicol, 2013, 57, 371-379. + 展開

參考文獻

[1] Qiu D, et al. J Biol Chem, 1999, 274(19), 13443-13450.
[2] Yang S, et al. Mol Cancer Ther, 2003, 2(1), 65-72.
[3] Lee KY, et al. J Biol Chem, 1999, 274(19), 13451-13455.

[4] Leuenroth SJ, et al. Proc Natl Acad Sci, 2007, 104(11), 4389-4394.
[5] Xu L, et al. Food Chem Toxicol, 2013, 57, 371-379.

+ 展開

化學信息&溶解度

分子量	360.4	分子式	C₂₀H₂₄O₆
CAS號	38748-32-2	SDF	Download Triptolide SDF
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 72 mg/mL ( (199.77 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 72 mg/mL ( (199.77 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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C1=C0/X	C1:	LOG(C1):
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C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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