This is a demo store. No orders will be fulfilled.

 
Call +1 (833) 552-7181 or Contact us
Toggle Nav
My Cart
Search
Advanced Search
Menu
Account
Settings
྾
main product photo

mTOR inhibitor-3 - 99%, high purity , CAS No.1207358-59-5

COA COA
    Grade & Purity:
  • ≥99%
In stock
Item Number
M647028
Grouped product items
SKU Size
Availability
 Price Qty
M647028-2mg
2mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$91.90
M647028-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$200.90
M647028-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$280.90
M647028-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$750.90
M647028-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,350.90
Wish List
Bulk Order  SDS  DATASHEET  Specification Sheet
View related series
mTOR (145) PI3K/Akt/mTOR (765)

Basic Description

Specifications & Purity ≥99%
Biochemical and Physiological Mechanisms mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a K i of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

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

In Vitro

mTOR inhibitor-3 (Compound 12i) inhibits mTOR with a K i of 1.5 nM, 500-fold selectivity over closely related PI3 kinases. mTOR inhibitor-3 inhibits NCI-PC3 and MCF7neo/Her2 cells proliferation with IC 50 s of 150 nM and 57 nM, respectively. 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) . 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 (t 1/2 =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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal administration

Mice Human prostate cancer NCI-PC3 cells are implanted subcutaneously into the right hind flanks of female NCR nude mice (5×10 6 cells in 100 μL of Hank’s balanced salt solution). Tumors are monitored until they reach a mean tumor volume of approximately 500 mm 3 . 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. aladdin has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

Associated Targets(Human)

CYP3A4 Tclin Cytochrome P450 3A4 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MTOR Tclin Serine/threonine-protein kinase mTOR (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MTOR Tclin Serine/threonine-protein kinase mTOR (13850 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PC-3 (62116 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HepG2 (196354 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Liver microsomes (16955 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Liver (3974 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MTOR Tclin mTORC1 (330 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Plasma (328 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Smiles CCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CCN(C3)C4=NC=CC=N4)C(=N2)N5CCOC[C@@H]5C
Isomeric SMILES CCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CCN(C3)C4=NC=CC=N4)C(=N2)N5CCOC[C@@H]5C
PubChem CID 59239114
Molecular Weight 474.56

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility DMSO : 50 mg/mL (105.36 mM; Need ultrasonic)
Molecular Weight 474.600 g/mol
XLogP3 2.100
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 8
Rotatable Bond Count 5
Exact Mass 474.249 Da
Monoisotopic Mass 474.249 Da
Topological Polar Surface Area 108.000 Ų
Heavy Atom Count 35
Formal Charge 0
Complexity 684.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 1
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

Reviews

Customer Reviews

Shall we send you a message when we have discounts available?

Remind me later

Thank you! Please check your email inbox to confirm.

Oops! Notifications are disabled.

Privacy Policy Website Terms of Use Return policy Terms and Conditions of Sale Cookie Policy Sales Policy
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Copyright © 2023-present Aladdin Scientific Corp . All rights reserved.