Torin 21223001-51-1

Torin2
分子式：C24H15F3N4O  分子量：432.4
 
產(chǎn)品描述
Torin 2是有效的，選擇性mTOR抑制劑，IC50為0.25 nM;作用于mTOR比作用于PI3K選擇性高800倍，且增強(qiáng)藥代動(dòng)力學(xué)特性，抑制ATM/ATR/DNA-PK，EC50分別為28 nM/35 nM/118 nM。
靶點(diǎn)
mTOR
         
IC50
0.25 nM
         
體外研究
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.Torin 2 inhibits mTORC1, thus activates TFEB by promoting its nuclear translocation with EC50 of 1.666 mM.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.
體內(nèi)研究
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.Torin 2(20mg/kg) ablates MYCN tumors with reduction in MYCN protein levels and induction of apoptosis in Th-MYCN mice.
溶解性
DMSO 20 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO