Torin 2

目錄號(hào)：S2817 Purity: 99.99%

Torin 2 是一種有效的選擇性mTOR抑制劑，在p53?/? MEFs細(xì)胞系中IC50為0.25 nM；作用于mTOR比作用于PI3K選擇性高800倍，并且改善了藥代動(dòng)力學(xué)性能。抑制ATM/ATR/DNA-PK，在PC3細(xì)胞系中EC50分別為28 nM/35 nM/118 nM。Torin 2 可降低細(xì)胞活力并誘導(dǎo)自噬與凋亡。

Torin 2 Chemical Structure

CAS: 1223001-51-1

規(guī)格	價(jià)格	庫存
10mM (1mL in DMSO)	1562.81	現(xiàn)貨
5mg	903.84	現(xiàn)貨
25mg	3030.61	現(xiàn)貨
50mg	4671.89	現(xiàn)貨
1g	24488.1	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.99%

99.99

Torin 2相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	mTORC1 mTORC2	點(diǎn)擊展開
相關(guān)產(chǎn)品	AZD8055 Torin 1 Ridaforolimus (Deforolimus, MK-8669) Sapanisertib (MLN0128) Torkinib (PP242) Vistusertib (AZD2014) MHY1485 KU-0063794 OSI-027 WYE-354 WYE-125132 (WYE-132) 3BDO Palomid 529 (P529) Zotarolimus (ABT-578) Salidroside GDC-0349 WAY-600 Onatasertib (CC 223) XL388 WYE-687	點(diǎn)擊展開
相關(guān)化合物庫	激酶抑制劑庫 PI3K/Akt 抑制劑庫凋亡分子化合物庫細(xì)胞周期化合物庫 NF-κB信號(hào)通路庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	孵育時(shí)間	活性描述	文獻(xiàn)信息
HCT116	Function assay	1 hr	Inhibition of mTORC1 in human HCT116 cells assessed as reduction in T389 phosphorylation on RPS6KB1 after 1 hr by Western blot analysis, EC50=0.00025μM	29211480
HEK293T	Function assay	20 mins	Inhibition of N-terminally FLAG-tagged mTORC1 (unknown origin) expressed in HEK293T cells using S6K1 or Akt1 as substrate after 20 mins by immunoblotting assay, IC50<0.01μM	29211480
HeLa	Function assay	20 mins	Inhibition of N-terminally FLAG-tagged mTORC2 (unknown origin) expressed in human HeLa cells using S6K1 or Akt1 as substrate after 20 mins by immunoblotting assay, IC50<0.01μM	29211480
RD	Antiviral assay	4 days	Antiviral activity against Enterovirus A71 infected in human RD cells assessed as reduction in virus-induced cell death incubated for 4 days by CellTiter-Glo luminescence assay, IC50=0.01μM	31082764
HCT116	Function assay	1 hr	Inhibition of ATM in human HCT116 cells assessed as after 1 hr by Western blot analysis, EC50=0.028μM	29211480
HCT116	Function assay	1 hr	Inhibition of ATR in human HCT116 cells assessed as after 1 hr by Western blot analysis, EC50=0.035μM	29211480
RD	Cytotoxicity assay	4 days	Cytotoxicity against human RD cells incubated for 4 days by CellTiter-Glo luminescence assay, CC50=0.04μM	31082764
HCT116	Function assay	1 hr	Inhibition of DNAPK in human HCT116 cells assessed as after 1 hr by Western blot analysis, EC50=0.118μM	29211480
MOLM13	Antiproliferative assay		Antiproliferative activity against human MOLM13 cells by Cell-Titer Glo assay, IC50<0.001μM	30370766
MOLM14	Antiproliferative assay		Antiproliferative activity against human MOLM14 cells by Cell-Titer Glo assay, IC50<0.001μM	30370766
MV4-11	Antiproliferative assay		Antiproliferative activity against human MV4-11 cells by Cell-Titer Glo assay, IC50<0.001μM	30370766
PC3	Function assay		Inhibition of PI3Kalpha in human PC3 cells expressing Akt1 S473D mutant assessed as phosphorylation of Akt Thr308 by immunoblotting, EC50=0.2μM	21322566
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
U-2 OS	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
Rh30	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
U-2 OS	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Rh18	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Rh30	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點(diǎn)

mTOR ^[1] (p53?/? MEFs)	ATM ^[5] (PC3 cells)	ATR ^[5] (PC3 cells)	DNA-PK ^[5] (PC3 cells)
0.25 nM	28 nM(EC50)	35 nM(EC50)	118 nM(EC50)

體外研究(In Vitro)
體外研究活性	Torin 2與PI3Kγ具有相同的結(jié)合模式，V882作為鉸鏈結(jié)合點(diǎn)，在內(nèi)部疏水袋Y867，D841 和D964再提供三個(gè)作用于氨基比林側(cè)鏈的氫鍵，類似于mTOR的Y2225，D2195 和D2357。^[1] Torin 2抑制mTORC1，因此通過促進(jìn)其核轉(zhuǎn)運(yùn)激活TFEB，EC50為1.666 mM。^[2] Torin 2(< 50 nM)引起MZ-CRC-1和TT細(xì)胞的活性顯著減少。Torin 2 (100 nM)使MZ-CRC-1和TT細(xì)胞的遷移顯著減少。^[3]
激酶實(shí)驗(yàn)	mTOR 和 PI3K 細(xì)胞試驗(yàn)
激酶實(shí)驗(yàn)	對(duì)mTOR的細(xì)胞IC50值使用p53?/? MEFs測(cè)定。細(xì)胞用載體或逐漸增減濃度的Torin 2處理1小時(shí)，然后裂解。S6K1 Thr-389的磷酸化使用磷酸-特異性抗體進(jìn)行免疫印跡監(jiān)測(cè)。同時(shí)，對(duì)PI3Ka的細(xì)胞IC50值，在p53?/?/mLST8?/?MEFs或表達(dá)S473D突變體Akt1的人PC3細(xì)胞中，基于Akt Thr-308的磷酸化進(jìn)行測(cè)定。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	MZ-CRC-1 和 TT 細(xì)胞
	濃度	50 nM
	孵育時(shí)間	3 天或 5 天
	方法	對(duì)于活性測(cè)定，MZ-CRC-1和TT細(xì)胞以一式四份接種在96孔板(1.0×10⁴細(xì)胞/孔)，培養(yǎng)基分別包含2.5%和4% FBS。24小時(shí)后，細(xì)胞用Torin 2處理。在指定時(shí)間點(diǎn)，細(xì)胞與10 μL CellTiter96 AQueous One溶液在100 μL培養(yǎng)基中培育3小時(shí)，吸光度在490 nm下測(cè)量。
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	PMID
	Western blot	p-S6K / S6K / p-AKT / AKT / IRS1 / p-4EBP1 / 4EBP1 / p-GSK3 p-Chk1 / Chk1 / p-Chk2 / Chk2 / p-DNA-PK		23436801
	Immunofluorescence	LC3B		23436801
	Growth inhibition assay	Cell viability		24434750

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在小鼠肝微粒體穩(wěn)定性試驗(yàn)中，Torin 2表現(xiàn)出>95%的藥效學(xué)響應(yīng)，和11.7分鐘的半衰期。Torin 2靜脈內(nèi)或口服給藥后，在雄性Swiss albino小鼠體內(nèi)表現(xiàn)出最好的生物利用度(51%)，短的半衰期(0.72小時(shí))和低清除率(19.6 mL/min/kg)。^[1] 在Th-MYCN 小鼠體內(nèi)，Torin 2(20mg/kg)消除MYCN腫瘤，減少M(fèi)YCN蛋白質(zhì)水平，并誘導(dǎo)細(xì)胞凋亡。^[4]
動(dòng)物實(shí)驗(yàn)	Animal Models	雄性 Swiss albino 小鼠
	Dosages	20 mg/kg
	Administration	靜脈內(nèi)或口服給藥

參考文獻(xiàn)
[1] Liu Q, et al. J Med Chem, 2011, 54(5), 1473-1480. [2] Settembre C, et al. EMBO J, 2012, 31(5), 1095-1108. [3] Tamburrino A, et al. Clin Cancer Res, 2012, 18(13), 3532-3540. [4] Berry T, et al. Cancer Cell, 2012, 22(1), 117-130. [5] Liu Q, et al. Cancer Res, 2013, 73(8), 2574-2586. + 展開

參考文獻(xiàn)

[1] Liu Q, et al. J Med Chem, 2011, 54(5), 1473-1480.
[2] Settembre C, et al. EMBO J, 2012, 31(5), 1095-1108.
[3] Tamburrino A, et al. Clin Cancer Res, 2012, 18(13), 3532-3540.

[4] Berry T, et al. Cancer Cell, 2012, 22(1), 117-130.
[5] Liu Q, et al. Cancer Res, 2013, 73(8), 2574-2586.

+ 展開

化學(xué)信息&溶解度

分子量	432.4	分子式	C₂₄H₁₅F₃N₄O
CAS號(hào)	1223001-51-1	SDF	Download Torin 2 SDF
Smiles	C1=CC(=CC(=C1)N2C(=O)C=CC3=CN=C4C=CC(=CC4=C32)C5=CN=C(C=C5)N)C(F)(F)F
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 30 mg/mL ( (69.38 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 30 mg/mL ( (69.38 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

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

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

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

第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)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(qǐng)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(jìn)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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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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