CZ415
- Product Name
- CZ415
- CAS No.
- 1429639-50-8
- Chemical Name
- CZ415
- Synonyms
- CZ415;CS-2392;CZ 415;CZ-415;CZ415 (Free base);CZ415, 10 mM in DMSO;inhibit,Inhibitor,mTOR,CZ415,CZ-415,CZ 415,Mammalian target of Rapamycin;(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-
- CBNumber
- CB83146695
- Molecular Formula
- C22H29N5O4S
- Formula Weight
- 459.56
- MOL File
- 1429639-50-8.mol
CZ415 Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
N-Bromosuccinimide Price
- Product number
- 27668
- Product name
- CZ415
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 27668
- Product name
- CZ415
- Packaging
- 25mg
- Price
- $586
- Updated
- 2024/03/01
- Product number
- 27668
- Product name
- CZ415
- Packaging
- 5mg
- Price
- $172
- Updated
- 2024/03/01
- Product number
- 27668
- Product name
- CZ415
- Packaging
- 10mg
- Price
- $321
- Updated
- 2024/03/01
- Product number
- C998985
- Product name
- CZ415
- Packaging
- 2.5mg
- Price
- $210
- Updated
- 2021/12/16
CZ415 Chemical Properties,Usage,Production
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.
in vivo
CZ415 is a highly selective mTOR inhibitor showing in vivo efficacy in a collagen induced arthritis (CIA) model. For full characterization of CZ415 and to enable improved dose predictions, the pharmacokinetic (PK) profile is assessed in rat. PK and oral bioavailability are determined after of 1 mg/kg intravenous (iv) bolus and 3 mg/kg oral (po) administration. The observed plasma clearance, corresponding to 45% liver blood flow, suggests that sufficient levels of free compound are circulating in the animal over time. The oral uptake is rapid with a Tmaxmax of 0.5 h and bioavailability F = 44% indicates very good absorption from the gut[1].
IC 50
mTOR: 8.07 (pIC50); mTORC1; mTORC2
References
[1] ANDREW D. CANSFIELD. CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model[J]. ACS Medicinal Chemistry Letters, 2016, 7 8: 768-773. DOI: 10.1021/acsmedchemlett.6b00149
[2] JING XIE. Targeting mTOR by CZ415 Inhibits Head and Neck Squamous Cell Carcinoma Cells.[J]. Cellular Physiology and Biochemistry, 2018, 46 2: 676-686. DOI: 10.1159/000488724
CZ415 Preparation Products And Raw materials
Raw materials
Preparation Products
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