1. PI3K/Akt/mTOR
  2. mTOR
  3. mTOR inhibitor-3

mTOR inhibitor-3 

Cat. No.: HY-18353 Purity: 98.54%
Handling Instructions

mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.

For research use only. We do not sell to patients.

mTOR inhibitor-3 Chemical Structure

mTOR inhibitor-3 Chemical Structure

CAS No. : 1207358-59-5

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 209 In-stock
Estimated Time of Arrival: December 31
5 mg USD 200 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.

IC50 & Target[2]

mTOR

1.5 nM (Ki)

mTORC1

 

mTORC2

 

In Vitro

mTOR inhibitor-3 (Compound 12i) inhibits mTOR with a Ki of 1.5 nM, 500-fold selectivity over closely related PI3 kinases. mTOR inhibitor-3 inhibits NCI-PC3 and MCF7neo/Her2 cells proliferation with IC50s of 150 nM and 57 nM, respectively[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

mTOR inhibitor-3 (Compound 8h) has high free plasma clearance in both mice (1818 mL/min/kg) and rats (1538 mL/min/kg in rat) [1]. mTOR inhibitor-3 (Compounds 12i) is selected for this study due to its potency, selectivity, and favorable mouse PK profile. Plasma levels of mTOR inhibitor-3 6 h following oral administration in PC3 tumor-bearing mice along with the fold decreases of phosphorylated mTORC1 and -2 substrates relative to time-matched vehicle controls. mTOR inhibitor-3 has moderate terminal elimination half-life (t1/2=1.7 h for mouse(1 mg/kg, iv)). mTOR inhibitor-3 achieves tumor stasis at the highest 200 mg/kg/day dose examined, which appears to also be approaching the limit of tolerability for this molecule[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

474.56

Formula

C₂₅H₃₀N₈O₂

CAS No.

1207358-59-5

SMILES

O=C(NC1=CC=C(C2=NC(N3[[email protected]@H](C)COCC3)=C4C(CN(C5=NC=CC=N5)CC4)=N2)C=C1)NCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (105.36 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1072 mL 10.5361 mL 21.0722 mL
5 mM 0.4214 mL 2.1072 mL 4.2144 mL
10 mM 0.2107 mL 1.0536 mL 2.1072 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.27 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.27 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

Mice[2]
Human prostate cancer NCI-PC3 cells are implanted subcutaneously into the right hind flanks of female NCR nude mice (5×106 cells in 100 μL of Hank’s balanced salt solution). Tumors are monitored until they reach a mean tumor volume of approximately 500 mm3. Then similarly sized tumors are randomly assigned to groups (n=4). Compounds are formulated as suspensions in 0.5% methylcellulose/0.2% Tween 80 (MCT) and dosed orally at 25, 50, and 100 mg/kg (100 μL dose/25 g animal). Tumor and plasma samples are harvested at 1, 6, and 10 h postdose.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

mTOR inhibitor-3mTOR inhibitor3mTOR inhibitor 3mTORMammalian target of RapamycinInhibitorinhibitorinhibit

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mTOR inhibitor-3
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HY-18353
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