Product Details
| Product Name:
MI-463 |
CAS No.:
1628317-18-9 |
| Purity:
99.28% |
Supply Ability:
10g |
| Release date:
2024/11/07 |
Product Introduction
Bioactivity
| 名稱 | MI-463 |
| 描述 | MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM). |
| 細(xì)胞實(shí)驗(yàn) | 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. |
| 動物實(shí)驗(yàn) | 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. |
| 體外活性 | 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. |
| 體內(nèi)活性 | 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. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 120 mg/mL (247.66 mM), Sonication is recommended.
|
| 關(guān)鍵字 | Epigenetic Reader Domain | Inhibitor | MI 463 | MI-463 | inhibit | MI463 |
| 相關(guān)產(chǎn)品 | ABBV-744 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | Tazemetostat | Piribedil | GSK126 | Curcumin | EPZ015666 | dBET6 | Naphthol AS-E | MRTX-1719 | Bisdemethoxycurcumin |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 表觀遺傳庫 | 染色質(zhì)修飾分子庫 | 抑制劑庫 | NO PAINS 化合物庫 | 口服活性化合物庫 | PPI抑制劑庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 共價抑制劑庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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