Torin 1
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Torin 1是一种有效的和选择性的mTOR激酶抑制剂,以ATP竞争的方式直接抑制包含mTOR的两个复合体mTORC1和mTORC2,IC50值分别为2 nM和10 nM。mTOR激酶是功能上完全不同的复合体mTORC1和mTORC2的催化亚单位,在调控细胞生长、增殖和存活方面起着至关重要的作用。据报道,Torin 1通过抑制mTORC1而非mTORC2,从而损害细胞生长和增值。同时,mTORC1的rapamycin抗性功能也被抑制。
参考文献:
[1]Thoreen CC1, Kang SA, Chang JW, Liu Q, Zhang J, Gao Y, Reichling LJ, Sim T, Sabatini DM, Gray NS. An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem. 2009 Mar 20;284(12):8023-32. doi: 10.1074/jbc.M900301200. Epub 2009 Jan 15.
[2]Liu Q1, Chang JW, Wang J, Kang SA, Thoreen CC, Markhard A, Hur W, Zhang J, Sim T, Sabatini DM, Gray NS. Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. J Med Chem. 2010 Oct 14;53(19):7146-55. doi: 10.1021/jm101144f.
- 1. Schwartz, Hannah, et al. "In vitro Methods to Better Evaluate Drug Responses in Cancer." UMass Chan Medical School. September 8, 2022.
- 2. Jordan E Hollembeak, Michael A Model. "Stability of Intracellular Protein Concentration under Extreme Osmotic Challenge." Cells. 2021 Dec 14;10(12):3532. PMID: 34944039
- 3. Holly Merta, Jake W. Carrasquillo Rodríguez, et al. "Cell cycle regulation of ER membrane biogenesis protects against chromosome missegregation." Dev Cell. 2021 Dec 20;56(24):3364-3379.e10. PMID: 34852214
- 4. Bikash Ranjan Sahoo. "HOST CELL RESPONSES TO ZIKA VIRUS INFECTION." University of Nebraska, August, 2021.
- 5. Yilei Zhang, Robert V Swanda, et al. "mTORC1 couples cyst(e)ine availability with GPX4 protein synthesis and ferroptosis regulation." Nat Commun. 2021 Mar 11;12(1):1589. PMID: 33707434
- 6. Bikash R. Sahoo, Aryamav Pattnaik, et al. "Mechanistic Target of Rapamycin (mTOR) Signaling Activation Antagonizes Autophagy to Facilitate Zika Virus Replication." J Virol 2020 Sep 2;JVI.01575-20. PMID: 32878890
- 7. Wang J, Chen Y, et al. "mTORC1-IRE1α pathway activation contributes to palmitate-elicited triglyceride secretion and cell death in hepatocytes." Exp Biol Med (Maywood). 2020;1535370220928276. PMID: 32436749
- 8. Martin-Hurtado A, Martin-Morales R, et al. "NRF2-dependent gene expression promotes ciliogenesis and Hedgehog signaling." Sci Rep. 2019 Sep 25;9(1):13896. PMID: 31554934
- 9. Zhang C, Duan Y, et al. "TFEB mediates immune evasion and resistance to mTOR inhibition of renal cell carcinoma via induction of PD-L1." Clin Cancer Res. 2019 Aug 5. pii: clincanres.0733.2019. PMID: 31383732
- 10. Rodríguez-Sánchez I, Schafer XL, et al. "The Human Cytomegalovirus UL38 protein drives mTOR-independent metabolic flux reprogramming by inhibiting TSC2." PLoS Pathog. 2019 Jan 24;15(1):e1007569. PMID: 30677091
- 11. Aline Pfefferle, Benedikt Jacobs, et al. "Intra-lineage Plasticity and Functional Reprogramming Maintain Natural Killer Cell Repertoire Diversity." bioRxiv. 2019 January 09. PMID: 30530705
- 12. Zhang Q, Presswalla F, et al. "A platform for assessing outer segment fate in primary human fetal RPE cultures." Exp Eye Res. 2018 Oct 15;178:212-222. PMID: 30336126
- 13. Admasu TD, Chaithanya Batchu K, et al. "Drug Synergy Slows Aging and Improves Healthspan through IGF and SREBP Lipid Signaling." Dev Cell. 2018 Oct 8;47(1):67-79.e5. PMID: 30269951
- 14. Wang K, Zhang T, et al."Identification of ANXA2 (annexin A2) as a specific bleomycin target to induce pulmonary fibrosis by impeding TFEB-mediated autophagic flux." Autophagy.2018;14(2):269-282. PMID: 29172997
- 15. Navid Koleini, Barbara E. Nickel, et al. "Fibroblast growth factor-2-mediated protection of cardiomyocytes from the toxic effects of doxorubicin requires the mTOR/Nrf-2/HO-1 pathway." Oncotarget.2017 August 24.
- 16. Jensen H, Potempa M, et al. "Cutting Edge: IL-2-Induced Expression of the Amino Acid Transporters SLC1A5 and CD98 Is a Prerequisite for NKG2D-Mediated Activation of Human NK Cells." J Immunol. 2017 Aug 7. pii: ji1700497. PMID: 28784848
Physical Appearance | A solid |
Storage | Desiccate at -20°C |
M.Wt | 607.64 |
Cas No. | 1222998-36-8 |
Formula | C35H28F3N5O2 |
Synonyms | Torin1;Torin-1 |
Solubility | insoluble in DMSO; insoluble in H2O; ≥2.42 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 1-[4-(4-propanoylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]-9-quinolin-3-ylbenzo[h][1,6]naphthyridin-2-one |
SDF | Download SDF |
Canonical SMILES | CCC(=O)N1CCN(CC1)C2=C(C=C(C=C2)N3C(=O)C=CC4=CN=C5C=CC(=CC5=C43)C6=CC7=CC=CC=C7N=C6)C(F)(F)F |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验: [1] | |
细胞系 |
MEFs |
制备方法 |
溶解度有限,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
反应条件 |
4 days,1-6 h |
实验结果 |
250 nM Torin1完全抑制细胞增殖,并诱导G1/S细胞周期停滞。此外,与50 nM rapamycin相比,250 nM Torin1使细胞大小降低到更大的程度。此外,与rapamycin相比,Torin1将mTORC1依赖的表型破坏的更充分。 |
动物实验: [2] | |
动物模型 |
U87-MG胶质母细胞瘤异种移植小鼠 |
给药剂量 |
每日一次,IP给药,20 mg/kg |
制备方法 |
以25 mg/mL溶于100%N-甲基-2-吡咯烷酮中 |
实验结果 |
Torin1连续治疗10天,抑制大于99%的肿瘤生长。治疗停止后肿瘤继续生长,表明Torin1主要是细胞抑制的,并且大量的肿瘤细胞在治疗期间仍然存活。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: 1. Thoreen CC, Kang SA, Chang JW et al. An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem. 2009 Mar 20;284(12):8023-32. 2. Liu Q, Chang JW, Wang J et al. Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benz o[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. J Med Chem. 2010 Oct 14;53(19):7146-55. |
描述 | Torin 1是一种有效的mTORC1/2抑制剂,IC50值分别为2 nM/10 nM。 | |||||
靶点 | mTOR | |||||
IC50 | 2-10 nM |
质量控制和MSDS
- 批次: