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Torin 1,mTOR抑制剂

高效的选择性mTOR抑制剂
规格或纯度: ≥97%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
T129642-5mg 5mg 现货 Stock Image
T129642-10mg 10mg 期货 Stock Image
T129642-25mg 25mg 现货 Stock Image
T129642-50mg 50mg 现货 Stock Image
T129642-100mg 100mg 现货 Stock Image

基本描述

规格或纯度 ≥97%
英文名称 Torin 1
别名 Torin-1
英文别名 Benzo[h]-1,6-naphthyridin-2(1H)-one, 1-[4-[4-(1-oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)-
生化机理 Torin 1 is potent and selective mTOR inhibitor (IC50 = 2 - 10 nM for mTORC1 and mTORC2). Torin1 displays 200-fold selectivity for mTOR over DNA-PK, ATM and hVps34.Potent, selective, ATP-competitive\xa0mTOR inhibitor that directly inhibits both mTORC1 and mTORC2 complexes, with IC 50 values between 2 and 10 nM in in vitro kinase assays. Displays 1000-fold selectivity for mTOR over PI3K, 200-fold selectivity for mTOR
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍


?Product Description:

Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.

名称和标识符

IUPAC Name 1-[4-(4-propanoylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]-9-quinolin-3-ylbenzo[h][1,6]naphthyridin-2-one
INCHI InChI=1S/C35H28F3N5O2/c1-2-32(44)42-15-13-41(14-16-42)31-11-9-26(19-28(31)35(36,37)38)43-33(45)12-8-24-20-40-30-10-7-22(18-27(30)34(24)43)25-17-23-5-3-4-6-29(23)39-21-25/h3-12,17-21H,2,13-16H2,1H3
InChi Key AKCRNFFTGXBONI-UHFFFAOYSA-N
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
分子式

C35H28F3N5O2

PubChem CID 49836027
分子量 607.62

化学和物理性质

溶解性 DMSO 2 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
敏感性 对光敏感

靶标

Target ID 2109
名称 mechanistic target of rapamycin kinase
缩写名 mTOR
家族 FRAP subfamily
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 2549 1p36.22 MTOR mechanistic target of rapamycin kinase
Mouse 2 2549 4 78.76 cM Mtor mechanistic target of rapamycin kinase
Rat 2 2549 5q36 Mtor mechanistic target of rapamycin kinase
Ensembl Gene ENSG00000198793 (Hs) , ENSMUSG00000028991 (Mm) , ENSRNOG00000009615 (Rn)
Entrez Gene 2475 (Hs) , 56717 (Mm) , 56718 (Rn)
OMIM 601231 (Hs)
UniProtKB P42345 (Hs) , P42346 (Rn) , Q9JLN9 (Mm)
RefSeq Nucleotide NM_004958 (Hs) , NM_019906 (Rn) , NM_020009 (Mm)
RefSeq Protein NP_004949 (Hs) , NP_063971 (Rn) , NP_064393 (Mm)
Protein GI 4826730 (Hs) , 227330586 (Mm) , 9845251 (Rn)
DrugBank Target P42345 (Hs)
CATH/Gene3D 1.10.1070.11 (N/A) , 1.20.120.150 (N/A) , 1.25.10.10 (N/A)
ChEMBL Target CHEMBL1075134 (Rn) , CHEMBL1255165 (Mm) , CHEMBL2842 (Hs)

关联配体

Ligand ID 8004
名称 torin 1
别名 Torin-1
类别 Synthetic organic
学名 1-[4-(4-propanoylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]-9-quinolin-3-ylbenzo[h][1,6]naphthyridin-2-one
生物活性评价 In assays using immuno-purified mTORC1 and mTORC2, torin 1 has an IC50 value of 2-10nM .
评价 Torin 1 is a potent inhibitor of mTOR in both mTOR containing protein complexes, mTORC1 and mTORC2. The discovery of torin 1 is described in , where it is compound 37.

参考文献

1. Thoreen CC, Kang SA, Chang JW, Liu Q, Zhang J, Gao Y, Reichling LJ, Sim T, Sabatini DM, Gray NS.  (2009)  An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1..  J Biol Chem,  284  (12):  (8023-32).  [PMID:19150980]
2. Liu Q, Chang JW, Wang J, Kang SA, Thoreen CC, Markhard A, Hur W, Zhang J, Sim T, Sabatini DM et al..  (2010)  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,  53  (19):  (7146-55).  [PMID:20860370]
3. Pe?ailillo J et al..  (2021)  Analysis of the early response to spinal cord injury identified a key role for mTORC1 signaling in the activation of neural stem progenitor cells..  NPJ Regen Med,  ():  (68).  [PMID:34686684]

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