Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CZ415 is a potent and highly selective mTOR inhibitor.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 13,500 | |||
5 mg | 在庫あり | ¥ 27,000 | |||
10 mg | 在庫あり | ¥ 43,000 | |||
25 mg | 在庫あり | ¥ 90,000 | |||
50 mg | 在庫あり | ¥ 136,000 | |||
100 mg | 在庫あり | ¥ 194,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 27,500 |
説明 | CZ415 is a potent and highly selective mTOR inhibitor. |
ターゲット&IC50 | mTOR:8.07(pIC50) |
In vitro | CZ415 shows no genotoxic potential and has very good cell permeability. Treatment of CZ415 leads to inhibition of phosphorylation for downstream targets of mTORC1 and mTORC2(IC50=14.5 nM for pS6RP and IC50=14.8 nM for pAKT). The immunosuppressive effect of CZ415 is measured by detecting secreted IFNγ after 18 h in stimulated human whole blood, and the resulting IC50 was 226 nM. CZ415 shows no genotoxic potential. It is neither mutagenic in a bacterial mutation assay (Ames test) nor does it show genotoxicity in the mouse lymphoma assay (MLA), in either the presence or absence of rat-liver S9 mix[1]. |
In vivo | In vivo studies show that CZ415 has moderate clearance and good oral bioavailability. In an anti-CD3 mouse model CZ415 efficiently inhibits mTOR downstream signaling and, in a CIA mouse model, shows significant antiinflammatory effects. With its extraordinary selectivity, drug-like properties and proven efficacy in vivo, CZ415 represents an ideal molecule for the pharmacological investigation of mTOR pathophysiological role in vivo[1]. |
細胞研究 | Cells are seeded in 90 μL DMEM containing 2% FCS at 4x104 cells/well (for pS6RP S240/244 assay) or 8x104 cells/well (for pAKT S473 assay) in a 96well U-bottom plate. The plate is then incubated for 1h in a humidified incubator (37oC, 5% CO2) to allow cells to adhere. CZ415: 3 μM start, 8 points 1:3 dilution steps, n=2. Positive control: 1 μM PI-103 (n=8). Negative control: DMSO (n=8). 10 μL of 10x compound concentration in 1% DMSO/99% (DMEM 2% FCS) are added to the cells followed by 2 h incubation in a humidified incubator (37oC, 5% CO2). Cells are lysed by addition of 10 μL 5x Complete Lysis Buffer and gentle shaking at 4°C for 15 min (Only for Reference) |
分子量 | 459.56 |
分子式 | C22H29N5O4S |
CAS No. | 1429639-50-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 84 mg/mL (182.8 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. 詳細
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CZ415 1429639-50-8 PI3K/Akt/mTOR signaling mTOR inhibit Inhibitor CZ-415 Mammalian target of Rapamycin CZ 415 inhibitor