mTOR-IN-1

Modify Date: 2024-01-05 18:28:07

mTOR-IN-1 structure	Common Name	mTOR-IN-1
	CAS Number	1207358-59-5	Molecular Weight	474.55800
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₅H₃₀N₈O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of mTOR-IN-1

mTOR-IN-1 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR-IN-1 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.

Name	1-ethyl-3-[4-[4-[(3S)-3-methylmorpholin-4-yl]-7-pyrimidin-2-yl-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea
Synonym	More Synonyms

Description	mTOR-IN-1 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR-IN-1 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
Related Catalog	Research Areas >> Cancer
Target	mTOR:1.5 nM (Ki) mTORC1 mTORC2
In Vitro	mTOR-IN-1 (Compound 12i) inhibits mTOR with a Ki of 1.5 nM, 500-fold selectivity over closely related PI3 kinases. mTOR-IN-1 inhibits NCI-PC3 and MCF7neo/Her2 cells proliferation with IC50s of 150 nM and 57 nM, respectively[2].
In Vivo	mTOR-IN-1 (Compound 8h) has high free plasma clearance in both mice (1818 mL/min/kg) and rats (1538 mL/min/kg in rat) [1]. mTOR-IN-1 (Compounds 12i) is selected for this study due to its potency, selectivity, and favorable mouse PK profile. Plasma levels of mTOR-IN-1 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-IN-1 has moderate terminal elimination half-life (t1/2=1.7 h for mouse(1 mg/kg, iv)). mTOR-IN-1 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].
Animal Admin	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.
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. [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.

Molecular Formula	C₂₅H₃₀N₈O₂
Molecular Weight	474.55800
Exact Mass	474.24900
PSA	111.89000
LogP	3.27020

mTOR inhibitor

CS-1383

mTOR-IN-1

DC Chemicals Limited
China
Product Name: mTOR-IN-1
Price: $268.8/10mg $724.8/50mg
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: MTOR inhibitor
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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Price: $343/10mM*1mLinDMSO

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mTOR-IN-1

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