Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 13,000 | |||
5 mg | 在庫あり | ¥ 22,500 | |||
10 mg | 在庫あり | ¥ 35,500 | |||
25 mg | 在庫あり | ¥ 64,000 | |||
50 mg | 在庫あり | ¥ 91,500 | |||
100 mg | 在庫あり | ¥ 123,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 22,500 |
説明 | MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM). |
In vitro | Treatment of murine bone marrow cells (BMC) transformed with the mLL-AF9 oncogene with MI-463 results in substantial growth inhibition (GI50: 0.23 μM). MI-463 is effective in inducing differentiation of MLL leukemia cells. Treatment with sub-micromolar concentrations of MI-463 also leads to markedly reduced expression of Hoxa9 and Meis1. |
In vivo | MI-463 shows substantial survival benefit in mouse models of MLL leukemia. It has very favorable druglike properties, including metabolic stability and PK profile in mice. MI-463 achieves high level in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability (45%). MI-463 induces strong inhibition of tumor growth with once-daily intraperitoneal (i.p.) administration. The expression of mLL fusion protein target genes, HOXA9 and MEIS1, is significantly reduced upon treatment with MI-463. |
細胞研究 | Leukemia cells are treated with MI-463 or 0.25% DMSO and cultured at 37 °C for 7 days. Media is changed on day 4, viable cell numbers are restored to the original concentration and MI-463 is re-supplied. MTT cell proliferation assay kit is then employed, and plates are read for absorbance at 570 nm using a microplate reader. |
動物実験 | For efficacy studies in MV4;11 subcutaneous xenograft mice model, 5×10^6 cells are injected into the 4-6 week old female BALB/c nude mice. Treatment is started when the tumor size reached ~100 mm^3. Vehicle (25% DMSO, 25% PEG400, 50% PBS) or MI-463 are administrated once daily at designated doses using i.p. injections. |
分子量 | 484.54 |
分子式 | C24H23F3N6S |
CAS No. | 1628317-18-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 120 mg/mL (247.66 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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MI-463 1628317-18-9 Chromatin/Epigenetic Epigenetic Reader Domain Histone Methyltransferase Inhibitor MI 463 inhibit MI463 inhibitor