BKT140
| 中文名称 | BKT140 |
|---|---|
| 中文同义词 | 化合物 T14665;莫替昔福特 (三氟乙酸盐);BKT140游离态;(3S,6S,9S,12R,17R,20S,23S,26S,29R,34AS)-N-((S)-1-氨基-5-胍基-1-氧代戊-2-基)-26,29-双(4-氨基丁基)-17-((S)-2-((S)-2-((S)-2-(4-氟苯甲酰氨基)-5-胍基戊酰氨基)-5-胍基戊酰氨基)-3-(萘-2-基)丙酰氨基)-6-(3-胍基丙基)-3,20-双(4-羟基苄基)-1,4,7,10,18,21,24,27,30-九氧代-9,23-双(3-脲基丙基)三十氢-1H,16H-吡咯并[2,1-P][1,2]二硫杂[5,8,11,14,17,20,23,26,29]九氮杂环三十二烷-12-甲酰胺;BL-8040|||BKT140 (4-FLUOROBENZOYL)|||TF14016;CXCR4拮抗剂;化合物 MOTIXAFORTIDE |
| 英文名称 | BL-8040 |
| 英文同义词 | BL-8040;BKT140;BKT140CXCR4 antagonist;BKT140 (BL-8040);BKT140 4-fluorobenzoyl;MOTIXAFORTIDE;BL-8040;TF14016;4F-Benzoyl-TN14003;BL-8040; TF14016; 4F-BENZOYL-TN14003 |
| CAS号 | 664334-36-5 |
| 分子式 | C97H144FN33O19S2 |
| 分子量 | 2159.52 |
| EINECS号 | |
| 相关类别 | 标准品;医药原料;贝尔卡主打 |
| Mol文件 | 664334-36-5.mol |
| 结构式 |  |
BKT140 性质
| 密度 | 1.52±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO 中≥216 mg/mL； ≥2.61 mg/mL，乙醇溶液，温和加热并超声；水中≥52.4 mg/mL |
| 形态 | 结晶固体 |
| 颜色 | 白色至米白色 |
Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) 是一种 CXCR4 的拮抗剂，IC50值约为1 nM。BL-8040 通过改变的miR-15a/16-1的表达，下调 ERK、BCL-2、MCL-1 和 cyclin-D1，诱导AML胚的凋亡。
| Target | Value |
|
ERK
() | |
|
Bcl-2
() | |
|
MCL-1
() | |
|
cyclin-D1
() | |
|
CXCR4
(Cell-free assay) | 1 nM |
Motixafortide (BKT140) displays selective toxicity toward AmL and MM cells. Treatment with Motixafortide (BKT140) can overcome IL-6 dependent proliferation and survival of ARH77 MM cells. Motixafortide (BKT140) specifically triggers CXCR4-dependent cell death in leukemia and MM cells. Motixafortide (BKT140) stimulates apoptotic cell death in leukemia and MM cells.
Subcutaneous injections of Motixafortide (BKT140) significantly reduces, in a dose-dependent manner, the growth of human acute myeloid leukemia and multiple myeloma xenografts. Tumors from animals treated with Motixafortide (BKT140) are smaller in size and weights, had larger necrotic areas and high apoptotic scores.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/11/08 | S9665 | BKT140 Motixafortide (BL-8040) | 664334-36-5 | 5mg | 3600.13元 |
| 2024/11/08 | S9665 | BKT140 Motixafortide (BL-8040) | 664334-36-5 | 25mg | 7770元 |