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产品名称 | mTOR ↓ ↑ | mTORC1 ↓ ↑ | mTORC2 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
AZD-8055 |
++++
mTOR (full length), IC50: 0.8 nM mTOR (truncated), IC50: 0.13 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 |
DNA-PK,PDGFR | 99%+ | ||||||||||||||||
Everolimus | 99%+ | ||||||||||||||||||
WYE-354 |
+++
mTOR, IC50: 5 nM |
98% | |||||||||||||||||
Tacrolimus | ✔ | 98% | |||||||||||||||||
PP121 |
++
mTOR, IC50: 13 nM |
VEGFR,PDGFR | 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。 |
靶点 |
|
描述 | Nordihydroguaiaretic acid (NDGA), a natural dicatechol, a selective 5LOX inhibitor, was one of the most potent non-cytotoxic antagonists tested (IC50 8 +/- 3 mM). Oral NDGA (2500 p.p.m.) significantly extended lifespan and slowed motor dysfunction in this mouse, when administration was begun relatively late in life (90 days). NDGA extended median total lifespan of G93A-SOD1 mice by 10%, and life expectancy following start of treatment was extended by 32%[3]. Feeding ob/ob mice a chow diet supplemented with either low (0.83 g/kg diet) or high-dose (2.5 g/kg diet) NDGA for 16 wk significantly improved plasma triglyceride (TG), inflammatory chemokine levels, hyperinsulinemia, insulin sensitivity, and glucose intolerance[4]. NDGA suppresses NRP1 function by downregulating its expression, which leads to attenuated cell motility, cell adhesion to ECM and FAK signaling in cancer cells. Moreover, due to its cross-cell type activity on NRP1 suppression, NDGA also impairs angiogenesis function of endothelial cells and fibronectin assembly by fibroblasts, both of which are critical to promote metastasis. NDGA effectively suppresses tumor metastasis in nude mice model[5]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02575794 | High Grade Glioma (III or IV) | Phase 1 | Recruiting | December 15, 2022 | United States, Alabama ... 展开 >> UAB Comprehensive Cancer Center Not yet recruiting Birmingham, Alabama, United States, 35294-3410 Contact: Thiru Pillay, RN 205-934-1842 thiru@uab.edu Principal Investigator: Burt Nabors, MD United States, California Jonsson Comprehensive Cancer Center at UCLA Not yet recruiting Los Angeles, California, United States, 90095 Contact: Timothy Cloughesy, MD 310-825-5321 TCloughesy@mednet.ucla.edu Principal Investigator: Timothy Cloughesy, MD United States, Maryland Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Recruiting Baltimore, Maryland, United States, 21231 Contact: Quinn qta@jhmi.edu, RN 410-955-8837 qta@jhmi.edu Contact: Trisha Surakus 410-502-9864 tsuraku1@jhmi.edu Sub-Investigator: Matthias Holdhoff, MD Principal Investigator: Stuart Grossman, MD United States, Massachusetts Dana Farber Cancer Institute Not yet recruiting Boston, Massachusetts, United States, 02215 Contact: Jennifer Barrs 617-632-6119 JenniferA_Barrs@DFCI.HARVARD.EDU Principal Investigator: Patrick Wen, MD United States, Michigan Josephine Ford Cancer Center at Henry Ford Hospital Recruiting Detroit, Michigan, United States, 48202 Contact: Amy Williamson, RN awillia12@hfhs.org Contact: Emily Krozek, MHSA Ekrozek1@hfhs.org Principal Investigator: Tobias Walbert, MD United States, North Carolina Wake Forest University Comprehensive Cancer Center Not yet recruiting Winston-Salem, North Carolina, United States, 27157 Contact: Clinical Trials Office 336-713-6771 Principal Investigator: Glenn Lesser, MD United States, Ohio Cleveland Clinic Taussig Cancer Center Not yet recruiting Cleveland, Ohio, United States, 44195 Contact: Cancer Center-Cares 216-444-7923 Sub-Investigator: David Peereboom, MD United States, Pennsylvania Abrams Cancer Center of the University of Pennsylvania Not yet recruiting Philadelphia, Pennsylvania, United States, 19104 Contact: Clinical Trials Office-Abrams Cancer Center 800-474-9892 Principal Investigator: Arati Desai, MD Hillman Cancer Center at University of Pittsburgh Cancer Institute Not yet recruiting Pittsburgh, Pennsylvania, United States, 15232 Contact: Clinical Trials Office - UPMC Cancer Centers 412-647-8073 Principal Investigator: Frank Lieberman, MD 收起 << |
NCT00664677 | Leukemias Acu... 展开 >>te Myeloid Leukemia (AML) Acute Lymphocytic Leukemia (ALL) Adult T Cell Leukemia (ATL) Chronic Myeloid Leukemia (CML-BP) Chronic Lymphocytic Leukemia (CLL) Myelodysplastic Syndrome (MDS) Chronic Myelomonocytic Leukemia (CMML) 收起 << | Phase 1 | Terminated(Funding constraints... 展开 >>) 收起 << | - | United States, North Carolina ... 展开 >> UNC, Lineberger Comprehensive Cancer Center Chapel Hill, North Carolina, United States, 27599 收起 << |
NCT00664586 | Refractory Solid Tumors ... 展开 >> Lymphoma 收起 << | Phase 1 | Terminated(Funding constraints... 展开 >>) 收起 << | - | United States, Tennessee ... 展开 >> The Sarah Cannon Cancer Center Nashville, Tennessee, United States, 37203 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.31mL 0.66mL 0.33mL |
16.54mL 3.31mL 1.65mL |
33.07mL 6.61mL 3.31mL |
CAS号 | 500-38-9 |
分子式 | C18H22O4 |
分子量 | 302.36 |
别名 | NDGA;NSC 4291 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Room Temperature |
溶解度 |
DMSO: 250 mg/mL(826.82 mM),配合低频超声助溶,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 |