Powder: -20°C for 3 years | In solvent: -80°C for 1 year
VU0661013 is an effective and selective inhibitor of MCL-1.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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1 mg | 在庫あり | ¥ 41,000 | |||
5 mg | 在庫あり | ¥ 104,500 | |||
10 mg | 在庫あり | ¥ 154,500 | |||
25 mg | 在庫あり | ¥ 243,500 | |||
50 mg | 在庫あり | ¥ 328,500 | |||
100 mg | 在庫あり | ¥ 441,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 112,500 |
説明 | VU0661013 is an effective and selective inhibitor of MCL-1. |
In vitro | VU0661013 does not obviously suppress BCL-xL (Ki>40 μM) or BCL-2 (Ki=0.73 μM). VU0661013 shows a Ki of 97±30 pM to human MCL-1 in a TR-FRET assay by displacing a fluorescently labeled peptide derived from the pro-apoptotic protein BAK [1]. |
In vivo | VU0661013 is a potent and selective MCL-1 inhibitor and is active in Venetoclax-resistant cells and patient-derived xenografts. VU0661013 treatment of disseminated human AML results in a dose-dependent decrease in tumor burden, nearly eliminating the hCD45+ MV-4-11 cells at the 75 mg/kg dose in the blood (mean, 13.0±2.2% in vehicle vs 7.4±7.2% in 25mg/kg vs 0.17±0.12% in 75 mg/kg treated mice), bone marrow (mean, 40.7±13.9% in vehicle vs 33.46±4.0 % in 25 mg/kg vs 0.384±0.345 in 75 mg/kg treated mice), and spleen (mean, 46.22±13.3% in vehicle vs 13.31±10.0% in 25 mg/kg vs 1.588±1.51% in 75 mg/kg treated mice). Treatment with VU0661013 reduces disease-associated splenomegaly (mean, vehicle vs. 75mg/kg, 0.17±0.02 vs 0.09±0.01g), and amending spleen to body weight ratio (vehicle vs 75mg/kg, 0.99 vs 0.50). In this study, NSGS mice are treated daily (starting 7 days after transplant) with vehicle only, 15 mg/kg or 75 mg/kg of VU0661013. Analysis reveals an increase in survival in mice treated with the 75mg/kg dose (vehicle treated mice=31 days, vs 15 mg/kg=32 days, vs 75 mg/kg treated mice=43 Days) [1]. |
別名 | VU661013 |
分子量 | 712.66 |
分子式 | C39H39Cl2N5O4 |
CAS No. | 2131184-57-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 117mg/mL (164.2mM)
You can also refer to dose conversion for different animals. 詳細
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VU0661013 2131184-57-9 Apoptosis BCL VU 661013 VU 0661013 VU661013 VU-661013 VU-0661013 Inhibitor inhibitor inhibit