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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1820889-23-3
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥877.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥269.0 |
| 规格： | 5 mg | 产品价格： | ￥960.0 |
| 规格： | 10 mg | 产品价格： | ￥1400.0 |
| 规格： | 25 mg | 产品价格： | ￥2375.0 |
| 规格： | 50 mg | 产品价格： | ￥3413.0 |
| 规格： | 100 mg | 产品价格： | ￥4663.0 |
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INCB-057643
CAS No. : 1820889-23-3
MCE 国际站：INCB-057643
产品活性：INCB-057643 是一种新型，口服生物可利用的 BET 抑制剂。
研究领域：Epigenetics | Apoptosis
作用靶点：Epigenetic Reader Domain | Apoptosis
In Vitro: INCB-057643 is a novel, orally bioavailable BET inhibitor. INCB-057643 inhibits binding of BRD2/BRD3/BRD4 to an acetylated histone H4 peptide in the low nM range, and is selective against other bromodomain containing proteins. In vitro analyses show that INCB-057643 inhibits proliferation of human AML, DLBCL, and multiple myeloma cell lines, with a corresponding decrease in MYC protein levels. Cell cycle analyses indicate that G1 arrest and a concentration-dependent increase in apoptosis are seen within 48 hours of treatment with INCB-057643.
In Vivo: Production of several cytokines, including IL-6, IL-10 and MIP-1α, is repressed by INCB-057643 in human and mouse whole blood stimulated ex vivo with LPS. Oral administration of INCB-057643 results in significant anti-tumor efficacy in xenograft models of AML, myeloma, and DLBCL. Additionally, combining INCB-057643 with standard of care agents used for the treatment of DLBCL including rituximab and bendamustine results in enhanced anti-tumor efficacy relative to that achieved with single agent therapies at doses that are well tolerated.
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