Torin 1是一种高效的 mTOR 抑制剂,其 IC50 为 3 nM,抑制 mTORC1 和 mTORC2 复合物的 IC50 值在 2 至 10 nM 之间,是一种有效的自噬诱导剂。
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产品名称 | mTOR ↓ ↑ | mTORC1 ↓ ↑ | mTORC2 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
AZD-8055 |
++++
mTOR (truncated), IC50: 0.13 nM mTOR (full length), IC50: 0.8 nM |
99%+ | |||||||||||||||||
Gedatolisib |
++++
mTOR, IC50: 1.6 nM |
98% | |||||||||||||||||
GSK1059615 |
++
mTOR, IC50: 12 nM |
98% | |||||||||||||||||
Vistusertib |
+++
mTOR, IC50: 2.8 nM |
99%+ | |||||||||||||||||
Torin 1 |
+++
mTOR, IC50: 4.32 nM |
+++
mTORC1, IC50: 2 nM |
++
mTORC2, IC50: 10 nM |
DNA-PK | 99%+ | ||||||||||||||
Dactolisib |
+++
mTOR (p70S6K), IC50: 6 nM |
98+% | |||||||||||||||||
PI-103 |
+
mTOR, IC50: 30 nM |
99%+ | |||||||||||||||||
WAY-600 |
++
mTOR, IC50: 9 nM |
99% | |||||||||||||||||
Voxtalisib |
+
mTOR, IC50: 157 nM |
99%+ | |||||||||||||||||
PF-04691502 |
++
mTOR, Ki: 16 nM |
98+% | |||||||||||||||||
Onatasertib |
++
mTOR, IC50: 16 nM |
DNA-PK | 99%+ | ||||||||||||||||
Chrysophanol | ✔ | EGFR | 98% | ||||||||||||||||
Samotolisib | ✔ | DNA-PK | 99%+ | ||||||||||||||||
Torkinib |
+++
mTOR, IC50: 8 nM |
PDGFR,DNA-PK | 99%+ | ||||||||||||||||
Everolimus | 99%+ | ||||||||||||||||||
WYE-354 |
+++
mTOR, IC50: 5 nM |
98% | |||||||||||||||||
Tacrolimus | ✔ | 98% | |||||||||||||||||
PP121 |
++
mTOR, IC50: 13 nM |
PDGFR,VEGFR | 99%+ | ||||||||||||||||
Torin 2 |
++++
mTOR, IC50: 0.25 nM |
DNA-PK | 99%+ | ||||||||||||||||
Rapamycin |
++++
mTOR, IC50: ~0.1 nM |
98% | |||||||||||||||||
GDC-0349 |
+++
mTOR, Ki: 3.8 nM |
98% | |||||||||||||||||
XL388 |
++
mTOR, IC50: 9.9 nM |
+++
mTORC1, IC50: 8 nM |
+
mTORC2, IC50: 166 nM |
99%+ | |||||||||||||||
WYE-687 |
+++
mTOR, IC50: 7 nM |
98+% | |||||||||||||||||
Apitolisib |
+
mTOR, Ki app: 17 nM |
98%+ | |||||||||||||||||
WYE-132 |
++++
mTOR, IC50: 0.19 nM |
99%+ | |||||||||||||||||
Sapanisertib |
++++
mTOR, Ki: 1.4 nM |
99%+ | |||||||||||||||||
BGT226 maleate | ✔ | 99%+ | |||||||||||||||||
ETP-46464 |
++++
mTOR, IC50: 0.6 nM |
DNA-PK | 98% | ||||||||||||||||
PI3K-IN-1 |
+
mTOR, IC50: 157 nM |
98+% | |||||||||||||||||
Zotarolimus |
+++
FKBP-12, IC50: 2.8 nM |
99+% | |||||||||||||||||
OSI-027 |
+++
mTOR, IC50: 4 nM |
+
mTORC1, IC50: 22 nM |
+
mTORC2, IC50: 65 nM |
99%+ | |||||||||||||||
Ridaforolimus |
++++
mTOR, IC50: 0.2 nM |
99%+ | |||||||||||||||||
Temsirolimus |
+
mTOR, IC50: 1.76 μM |
95% | |||||||||||||||||
CZ415 |
++
mTOR, pIC50: 8.07 |
99%+ | |||||||||||||||||
SF2523 |
+
mTOR, IC50: 280 nM |
DNA-PK | 99%+ | ||||||||||||||||
KU-0063794 |
++
mTORC1, IC50: ~10 nM |
++
mTORC2, IC50: ~10 nM |
99%+ | ||||||||||||||||
Omipalisib |
++++
mTORC1, Ki: 0.18 nM |
++++
mTORC2, Ki: 0.3 nM |
99%+ | ||||||||||||||||
Palomid 529 | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SBI-0206965 |
+++
ULK1, IC50: 108 nM ULK2, IC50: 711 nM |
97% | |||||||||||||||||
Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
MRT68921 hydrochloride |
++++
ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM |
99%+ | |||||||||||||||||
ROC-325 | ✔ | 99%+ | |||||||||||||||||
Autophinib |
+++
Autophagy, IC50: 40 nM |
97% | |||||||||||||||||
Lys05 | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | In wild-type MEFs, Torin1 (250 nM) fully arrests proliferation, induces G1/S cell cycle arrest, and reduces cell size more significantly than 50 nM rapamycin[1]. Torin1 exhibits over 800-fold selectivity for mTOR over PI3Kis, demonstrating high specificity compared to other PIKK family kinases, except for DNA-PK[2]. |
体内研究 | Torin1 (20 mg/kg, i.p.) shows efficacy in a U87MG xenograft model, displaying significant pharmacodynamic inhibition of downstream effectors of mTOR in both tumor and peripheral tissues[2]. |
体外研究 | In wild-type MEFs, Torin1 (250 nM) fully arrests proliferation, induces G1/S cell cycle arrest, and reduces cell size more significantly than 50 nM rapamycin[1]. Torin1 exhibits over 800-fold selectivity for mTOR over PI3Kis, demonstrating high specificity compared to other PIKK family kinases, except for DNA-PK[2]. |
作用机制 | Torin 1 is an ATP-competitive inhibitor. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
697 | Growth Inhibition Assay | IC50=0.00634 μM | SANGER | ||
8-MG-BA | Growth Inhibition Assay | IC50=0.04629 μM | SANGER | ||
A101D | Growth Inhibition Assay | IC50=0.0265 μM | SANGER | ||
A253 | Growth Inhibition Assay | IC50=0.98885 μM | SANGER | ||
Dose | Mice: 1 mg/kg[3] (i.v.), 10 mg/kg[3] (i.p./p.o.), 20 mg/kg[3] (i.p.) | ||||||||||||||||||||
Administration | i.v., i.p., p.o. | ||||||||||||||||||||
Pharmacokinetics |
|
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.65mL 0.33mL 0.16mL |
8.23mL 1.65mL 0.82mL |
16.46mL 3.29mL 1.65mL |
CAS号 | 1222998-36-8 |
分子式 | C35H28F3N5O2 |
分子量 | 607.624 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 2 mg/mL(3.29 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |