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ChemicalBook--->CAS DataBase List--->1429639-50-8

1429639-50-8

1429639-50-8 Structure

1429639-50-8 Structure
IdentificationBack Directory
[Name]

CZ415
[CAS]

1429639-50-8
[Synonyms]

CZ415
CS-2392
CZ 415;CZ-415
CZ415 (Free base)
(S)-1-(4-(7,7-dimethyl-4-(3-methylmorpholino)-6,6-dioxido-5,7-dihydrothieno[3,4-d]pyrimidin-2-yl)phenyl)-3-ethylurea
Urea, N-[4-[5,7-dihydro-7,7-dimethyl-4-[(3S)-3-methyl-4-morpholinyl]-6,6-dioxidothieno[3,4-d]pyrimidin-2-yl]phenyl]-N'-ethyl-
[EINECS(EC#)]

604-604-1
[Molecular Formula]

C22H29N5O4S
[MDL Number]

MFCD30533321
[MOL File]

1429639-50-8.mol
[Molecular Weight]

459.56
Chemical PropertiesBack Directory
[Boiling point ]

611.4±55.0 °C(Predicted)
[density ]

1.287±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO:73.67(Max Conc. mg/mL);160.3(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:6):0.1(Max Conc. mg/mL);0.22(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);65.28(Max Conc. mM)
Ethanol:10.0(Max Conc. mg/mL);21.76(Max Conc. mM)
[form ]

A crystalline solid
[pka]

13.79±0.46(Predicted)
[color ]

White to off-white
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H315-H335-H319
[Precautionary statements ]

P264-P280-P305+P351+P338-P337+P313P-P264-P280-P302+P352-P321-P332+P313-P362
Hazard InformationBack Directory
[Description]

CZ415 is an inhibitor of mammalian target of rapamycin (mTOR; Kd = 6.3 nM). It is 1,000-fold selective for mTOR over a panel of 285 kinases. CZ415 inhibits phosphorylation of S6 ribosomal protein (S6RP) and Akt in HEK293T cells (IC50s = 14.5 and 14.8 nM, respectively). It inhibits IFN-γ secretion in IL-2, anti-CD3, and anti-CD28 antibody-stimulated human whole blood (IC50 = 226 nM). CZ415 (10 mg/kg) reduces fore paw joint erythema and swelling in a mouse model of collagen-induced arthritis. It also inhibits intratumor mTOR activity and reduces tumor growth in an OCC-1 oral cavity carcinoma mouse xenograft model when administered at a dose of 20 mg/kg.
[Uses]

CZ415 is a selective and potent ATP-competitive mTOR inhibitor (1). It demonstrated in vivo efficacy in a semitherapeutic collagen induced arthritis (CIA) mouse model.
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