| Identification | Back 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 Properties | Back 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 |
| Hazard Information | Back 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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