1223001-51-1
Torin 2
CAS: 1223001-51-1
Molecular Formula: C24H15F3N4O
1223001-51-1 - Names and Identifiers
1223001-51-1 - Physico-chemical Properties
| Molecular Formula | C24H15F3N4O |
| Molar Mass | 432.4 |
| Density | 1.427 |
| Melting Point | >275° C (dec.) |
| Boling Point | 623.7±55.0 °C(Predicted) |
| Solubility | DMSO 20 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
| Appearance | White to beige powder |
| Color | white to beige |
| pKa | 5.66±0.26(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | 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. Torin 2 has the same binding mode as PI3Kγ, V882 acts as a hinge junction, providing three hydrogen bonds to aminopyrine side chain in inner hydrophobic bags Y867,D841 and d964, similar to Y2225,D2195 and D2357 of mTOR. Torin 2 inhibits mTORC1 and therefore activates TFEB by promoting its nuclear transport with an EC50 of 1.666 mM. Torin 2(< 50 nM) caused a significant reduction in the activity of MZ-CRC-1 and TT cells. Torin 2 (100 nM) significantly reduced the migration of MZ-CRC-1 and TT cells. |
| In vivo study | 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. Torin 2(20mg/kg) abrates MYCN tumors with reduction in MYCN protein levels and induction of apotosis in Th-MYCN mice. In a mouse liver microsomal stability assay, Torin 2 exhibited a pharmacodynamic response of> 95%, and a half-life of 11.7 minutes. Torin 2 showed the best bioavailability (51%) and short half-life (0.72 hours) in male Swiss albino mice after intravenous or oral administration and low clearance (19.6/min/kg). In Th-MYCN mice, Torin 2(20mg/kg) eliminated MYCN tumors, reduced MYCN protein levels, and induced apoptosis. |
1223001-51-1 - Introduction
Torin 2 is an effective and selective mTOR inhibitor with IC50 of 0.25 nM. The selectivity of mTOR acting on mTOR is 800 times higher than that of PI3K, and it enhances pharmacokinetic characteristics and inhibits ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM respectively.
Last Update：2022-10-16 17:41:21
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