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475990

mTOR Inhibitor IV, Ku-63794

The mTOR Inhibitor IV, Ku-63794, also referenced under CAS 938440-64-3, controls the biological activity of mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

mTOR Inhibitor IV, Ku-63794, rel-5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol, Ku-0063794, mTOR Inhibitor IV, Ku-63794

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About This Item

Empirical Formula (Hill Notation):
C25H31N5O4
CAS Number:
938440-64-3
Molecular Weight:
465.54
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD11977741
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

100

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

pale yellow

solubility

DMSO: 15 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

N5(C[C@H](O[C@H](C5)C)C)c1nc2nc(ccc2c(n1)N4CCOCC4)c3cc(c(cc3)OC)CO

InChI

1S/C25H31N5O4/c1-16-13-30(14-17(2)34-16)25-27-23-20(24(28-25)29-8-10-33-11-9-29)5-6-21(26-23)18-4-7-22(32-3)19(12-18)15-31/h4-7,12,16-17,31H,8-11,13-15H2,1-3H3/t16-,17+

InChI key

RFSMUFRPPYDYRD-CALCHBBNSA-N

General description

A cell-permeable pyrido-pyrimidine compound that acts as a highly selective and potent inhibitor against both mTORC1 & mTORC2 (IC50 = ~10 nM against mTOR activity in raptor or rictor immunoprecipitate from HEK293 with 100 µM ATP), with much reduced potency against MKK1 and PI 3-Kα (IC50 ~9 µM) and little or no activity toward more than 200 other protein and lipid kinases, including Akt, ATR, DNA-PK, PDK1, and PI 3-Kβ/γ/δ. Shown to effectively inhibit cellular mTOR phosphorylation on Ser2448/2481 as well as the phosphorylation and activation of mTORC1/2 downstream effector molecules such as Akt, S6K, 4E-BP1, but not RSK or Erk1/2, kinases that are not regulated by mTOR. Although Ku-63794 is shown not to affect IGF-1-induced Akt phosphorylation on Ser308 by PDK1 in mTORC2 knockout MEF cultures, Ku-63794 treatment of mTORC2-expressing MEF cells is shown to inhibit IGF-1-induced Akt Ser308 phosphorylation.

Packaging

Packaged under inert gas

Other Notes

Malagu, K., et al. 2009. Bioorg. Med. Chem. Lett.19, 5950.
Garcia-Martinez, J.M., et al. 2009. Biochem. J.421, 29.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

475990-MG: + 475990-5MG:

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Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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