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Torin 2

Torin 2

品 牌 MCE
C A S 号 1223001-51-1
货 号 HY-13002
规 格 10mg
价 格(元) 1252.00
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货号 规格 价格
HY-13002 10mg 1252.00
HY-13002 50mg 4201.00
HY-13002 100mg 5924.00

产品说明


Torin 2是高活性mTOR选择性抑制剂,IC50为0.25 nM,比对PI3K的抑制性强800倍,有较好的药代动力学特性,还能抑制ATM,ATR和DNA-PK,EC50分别为28 nM,35 nM和118 nM。



Torin 2的生物活性


Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties; inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM, respectively.
IC50 value: 0.25 nM [1]
Target: mTOR
in vitro: Torin 2 has the same binding mode as PI3Kγ, V882 serves as a hinge binding point and in the inner hydrophobic pocket Y867, D841 and D964 provide three more hydrogen bonds with aminopyridine side chain analogous to Y2225, D2195 and D2357 of mTOR [1]. Torin 2 inhibits mTORC1, thus activates TFEB by promoting its nuclear translocation with EC50 of 1.666 uM [2]. Torin 2(< 50 nM) causes a significant reduction in viability of both MZ-CRC-1 and TT cells. Torin 2 (100 nM) exerts a significant reduction of migration of both MZ-CRC-1 and TT cells [3].
in vivo: Torin 2 exhibits >95% pharmacodynamic response and half-time of 11.7 min in the mouse liver microsome stability study. Torin 2 exhibits the best bioavailability (51%), short half-life (0.72 hours) and low clearance(19.6 mL/min/kg) in male Swiss albino mice following intravenous and oral administration [1]. Torin 2(20mg/kg) ablates MYCN tumors with reduction in MYCN protein levels and induction of apoptosis in Th-MYCN mice [4].

化学信息


分子量 432.4 储存条件 参考CoA中推荐的条件进行储存。
分子式 C₂₄H₁₅F₃N₄O
CAS号 1223001-51-1
溶剂/溶解度 10 mM in DMSO

相关文献


[1]. Liu Q, et al. Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer. J Med Chem, 2011, 54(5), 1473-1480.
[2]. Settembre C, et al. A lysosome-to-nucleus signalling mechanism senses and regulates the lysosome via mTOR and TFEB. EMBO J, 2012, 31(5), 1095-1108.
[3]. Tamburrino A, et al. Activation of the mTOR pathway in primary medullary thyroid carcinoma and lymph node metastases. Clin Cancer Res, 2012, 18(13), 3532-3540.
[4]. Berry T, et al. The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma. Cancer Cell, 2012, 22(1), 117-130.