Name: Torin 2
Brand: Selleck Chemicals
SKU: S2817
Rating: 5 (70 reviews)

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품질 관리

배치: 순도: 99.7582%

99.7582

관련 타겟	PI3K Akt GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
기타 mTOR 억제제	Torin 1 AZD8055 Ridaforolimus (Deforolimus, MK-8669) Sapanisertib (MLN0128, INK-128) Torkinib (PP242) MHY1485 Vistusertib (AZD2014) KU-0063794 OSI-027 WYE-354

세포 배양, 처리 및 작업 농도

세포주	분석 유형	배양 시간	활성 설명	PMID
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
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
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
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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	432.4	화학식	C₂₄H₁₅F₃N₄O	보관 (수령일로부터)	3년-20°C분말
CAS 번호	1223001-51-1	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	C1=CC(=CC(=C1)N2C(=O)C=CC3=CN=C4C=CC(=CC4=C32)C5=CN=C(C=C5)N)C(F)(F)F

용해도

In vitro
배치:

DMSO : 30 mg/mL (69.38 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 41 mg/mL (94.81 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 30 mg/mL (69.38 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 41 mg/mL (94.81 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 30 mg/mL (69.38 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	1.500mg/ml (3.47mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

Targets/IC₅₀/Ki	mTOR (p53−/− MEFs) 0.25 nM ATM (PC3 cells) 28 nM(EC50) ATR (PC3 cells) 35 nM(EC50) DNA-PK (PC3 cells) 118 nM(EC50)
시험관 내(In vitro)	Torin 2는 PI3Kγ와 동일한 결합 모드를 가지며, V882는 힌지 결합점으로 작용하고 내부 소수성 포켓에서 Y867, D841 및 D964는 mTOR의 Y2225, D2195 및 D2357과 유사하게 아미노피리딘 측쇄와 3개의 추가 수소 결합을 제공합니다. 이 화합물은 mTORC1을 억제하여 TFEB의 핵 전위를 촉진함으로써 TFEB를 활성화하며 EC50은 1.666mM입니다. 이 화학물질(< 50nM)은 MZ-CRC-1 및 TT 세포 모두의 생존력을 유의하게 감소시킵니다. 이 물질(100nM)은 MZ-CRC-1 및 TT 세포 모두의 이동을 유의하게 감소시킵니다.
키나아제 분석	mTOR 및 PI3K 세포 분석
키나아제 분석	mTOR의 세포 IC50 값은 p53 / - MEF를 사용하여 결정됩니다. 세포는 1시간 동안 운반체 또는 증가하는 농도의 Torin 2로 처리된 후 용해됩니다. S6K1 Thr-389의 인산화는 인산화-특이적 항체를 사용한 면역블로팅으로 모니터링됩니다. 한편, PI3Ka의 세포 IC50 값은 p53 / /mLST8 / - MEF 또는 Akt1의 S473D 돌연변이를 발현하는 인간 PC3 세포에서 Akt Thr-308의 인산화를 기반으로 결정됩니다.
생체 내(In vivo)	Torin 2는 마우스 간 마이크로솜 안정성 연구에서 95% 이상의 약력학적 반응과 11.7분의 반감기를 보입니다. 이 화합물은 수컷 스위스 알비노 마우스에서 정맥 및 경구 투여 후 최고의 생체 이용률(51%), 짧은 반감기(0.72시간) 및 낮은 청소율(19.6mL/min/kg)을 보입니다. 이 화학물질(20mg/kg)은 Th-MYCN 마우스에서 MYCN 단백질 수준 감소 및 Apoptosis 유도를 통해 MYCN 종양을 제거합니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/21322566/ [2] https://pubmed.ncbi.nlm.nih.gov/22343943/ [3] https://pubmed.ncbi.nlm.nih.gov/22753663/ [4] https://pubmed.ncbi.nlm.nih.gov/22789543/ [5] https://pubmed.ncbi.nlm.nih.gov/23436801/

적용 분야

방법	바이오마커	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