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Merck

475991

Torin1

≥99% (HPLC), powder, mTOR inhibitor, Calbiochem®

別名:

mTOR Inhibitor XI, Torin1, 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one, DNA-PK Inhibitor VI, PI 3-K Inhibitor XVIII

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この商品について

実験式（ヒル表記法）:
C35H28F3N5O2
CAS番号:
1222998-36-8
分子量:
607.62
MDL number:
MFCD18782653
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥99% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
OK to freeze, protect from light

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製品名

mTOR Inhibitor XI, Torin1, mTOR Inhibitor XI, Torin1, CAS 1222998-36-8, is a cell-permeable, highly potent, ATP-competitive inhibitor of mTOR and DNA-PK (IC50 = 4.32 and 6.34 nM, respectively).

SMILES string

FC(F)(F)c1c(ccc(c1)[n]3c4c5c(ncc4cc[c]3=O)ccc(c5)c6cnc7c(c6)cccc7)N2CCN(CC2)C(=O)CC

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

assay

≥99% (HPLC)

form

powder

potency

2 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

yellow-white

solubility

DMSO: 2 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

関連するカテゴリー

General description

A cell-permeable pyridinonequinoline derivative that acts as a highly potent, ATP-competitive inhibibitor against mTOR and DNA-PK (IC50 = 4.32 and 6.34 nM, respectively, in cell-free kinase assays), inhibiting class I (IC50 =171, 250, and 564 nM, respectively, against P110γ, P110α/P85α, and P110δ/P85α, respectively), class II (IC50 =176 and 564 nM, respectively, against C2α, and C2β, respectively), and class III (IC50 = 533 nM against hVPS34) PI 3-K only at much higher concentrations. Effectively inhibits mTORC1-mediated S6K1 Thr389 phosphorylation in MEF cultures (IC50 = 2 nM) in vitro, as well as mTORC2-mediated Akt Ser473 and mTORC1-dependent S6 Ser235/236 phosphorylations in murine lung and liver in vivo (up to 6 h after single i.p. dose at 20 mg/kg). Despite its poor in vivo stability (T1/2 = 4.52 h in mice; 10 mg/kg i.p.), Torin1 is reported to completely suppress U87MG-derived tumor expansion in mice when administered via daily i.p. at a high dosage of 200 mg/kg. Also reported to effectively inhibit cellular mTORC1 functionalities known to be rapamycin-resistant (Cat. Nos. 553210, 553211, and 553212M).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
MTOR
Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20&degC). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Liu, Q., et al. 2010. J Med Chem.53, 7146.
Thoreen, C., et al. 2009. J Biol Chem.284, 8023.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

保管分類

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

475991-10MG: + 475991-MG:

jan

試験成績書（COA）

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以前この製品を購入いただいたことがある場合

文書ライブラリで、最近購入した製品の文書を検索できます。

文書ライブラリにアクセスする

Yucel Aydin et al.
Journal of hepatocellular carcinoma, 8, 1579-1596 (2021-12-18)
Hepatocellular carcinoma (HCC) developing in the context of preexisting cirrhosis is characterized by impaired autophagy that results in increased exosome release. This study was conducted to determine whether circulating exosomes expressing glypican 3 (GPC3) could be utilized as a biomarker
Takafumi Miyamoto et al.
Cell reports methods, 1(4), 100052-100052 (2022-04-28)
Engineered synthetic biomolecular devices that integrate elaborate information processing and precisely regulate living cell behavior have potential in various applications. Although devices that directly regulate key biomolecules constituting inherent biological systems exist, no devices have been developed to control intracellular
Manasa P Srikanth et al.
Stem cells translational medicine, 10(7), 1081-1094 (2021-03-04)
Gaucher disease (GD) is a lysosomal storage disorder caused by mutations in GBA1, the gene that encodes lysosomal β-glucocerebrosidase (GCase). Mild mutations in GBA1 cause type 1 non-neuronopathic GD, whereas severe mutations cause types 2 and 3 neuronopathic GD (nGD). GCase deficiency
Jee-Yun Park et al.
Scientific reports, 11(1), 21119-21119 (2021-10-28)
Transcription factor EB (TFEB) is a master regulator of the autophagy-lysosomal pathway (ALP). Here, we cloned a novel splicing variant of TFEB, comprising 281 amino acids (hereafter referred to as small TFEB), and lacking the helix-loop-helix (HLH) and leucine zipper
Carolyn-Ann Robinson et al.
PLoS pathogens, 19(1), e1011080-e1011080 (2023-01-13)
Kaposi's sarcoma-associated herpesvirus (KSHV) causes the inflammatory and angiogenic endothelial cell neoplasm, Kaposi's sarcoma (KS). We previously demonstrated that the KSHV Kaposin B (KapB) protein promotes inflammation via the disassembly of cytoplasmic ribonucleoprotein granules called processing bodies (PBs). PBs modify
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グローバルトレードアイテム番号

カタログ番号GTIN
475991-10MGCN04055977184433

ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.

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