| Identification | Back Directory | [Name]
MTOR inhibitor | [CAS]
1207358-59-5 | [Synonyms]
MTOR-IN-1
MTOR inhibitor
mTOR inhibitor-3
GDC-mTOR inhibitor
mTOR inhibitor (mTOR-IN-1)
Inhibitor,inhibit,mTOR,mTOR inhibitor 3,mTOR inhibitor-3,mTOR inhibitor3,Mammalian target of Rapamycin
N-Ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(2-pyrimidinyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea
Urea, N-ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(2-pyrimidinyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]- | [Molecular Formula]
C25H30N8O2 | [MDL Number]
MFCD25977126 | [MOL File]
1207358-59-5.mol | [Molecular Weight]
474.56 |
| Chemical Properties | Back Directory | [density ]
1.277±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 50 mg/mL (105.36 mM; Need ultrasonic) | [form ]
Powder | [pka]
13.87±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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. | [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]. | [IC 50]
mTOR: 1.5 nM (Ki); mTORC1; mTORC2 | [References]
[1] Pei Z, et al. Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349. ACS Med Chem Lett. 2012 Nov 29;4(1):103-7. DOI:10.1021/ml3003132
[2] Koehler MF, et al. Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity. J Med Chem. 2012 Dec 27;55(24):10958-71. DOI:10.1021/jm301389h |
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| Company Name: |
LETOPHARM LIMITED
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| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
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