AZD3965
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- CAS号:
- 1448671-31-5
- 英文名:
- AZD3965
- 英文别名:
- CS-2201;AZD-3965;AZD3965;AZD 3965;AZD3965,inhibit,Inhibitor,Monocarboxylate Transporter;(S)-5-(4-hydroxy-4-methylisoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-((5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)methyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione;5-{[(4S)-4-Hydroxy-4-methyl-1,2-oxazolidin-2-yl]carbonyl}-1-isopropyl-3-methyl-6-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl}thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione;5-[[(4S)-4-Hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione;Thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione, 5-[[(4S)-4-hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-
- 中文名:
- AZD3965
- 中文别名:
- 化合物AZD3965;(S)-5-(4-羟基-4-甲基异恶唑烷-2-羰基)-1-异丙基-3-甲基-6-((5-甲基-3-(三氟甲基)-1H-吡唑-4-基)甲基)噻吩并[2,3-D]嘧啶-2,4(1H,3H)-二酮
- CBNumber:
- CB63034312
- 分子式:
- C21H24F3N5O5S
- 分子量:
- 515.51
- MOL File:
- 1448671-31-5.mol
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AZD3965化学性质
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沸点:
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723.1±70.0 °C(Predicted)
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密度:
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1.483±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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insoluble in H2O; ≥51.5 mg/mL in DMSO; ≥51.6 mg/mL in EtOH
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形态:
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A crystalline solid
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酸度系数(pKa):
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10.92±0.50(Predicted)
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颜色:
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White to off-white
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AZD3965性质、用途与生产工艺
AZD3965是一种有效的,选择性的,口服的单羧酸盐转运蛋白1(MCT1)抑制剂,结合亲和力为1.6 nM,是MCT2的6倍。
在携带COR-L103异种移植物的非肥胖糖尿病scid-γ小鼠中,AZD3965(100 mg/kg,p.o.)减少肿瘤生长并增加肿瘤内乳酸。 在患有H526肿瘤的小鼠中,AZD3965(100 mg / kg,p.o.)引起乳酸浓度增加,生长减少和辐射敏感性增加。
在优先表达MCT1的淋巴瘤细胞系中,AZD3965有效抑制乳酸转运和细胞生长。 AZD3965抑制细胞中的MCT1活性,并在缺氧时显示更高的敏感性。 在H526,HGC27细胞和DMS114细胞中,AZD3965增加细胞内乳酸盐并显着降低乳酸盐摄取。
AZD3965是一种高效的,选择性的并且具有口服活性的monocarboxylate transporter 1 (MCT1)抑制剂,其结合亲和力为1.6 nM,比MCT2高6倍的选择性。Phase 1。
AZD3965
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/08/19 | S7339 | AZD3965 AZD3965 | 1448671-31-5 | 1mg | 795.14元 |
2024/08/19 | S7339 | AZD3965 AZD3965 | 1448671-31-5 | 5mg | 1613.67元 |
1448671-31-5, AZD3965 相关搜索:
- 药靶配体
- 抑制剂
- (S)-5-(4-羟基-4-甲基异恶唑烷-2-羰基)-1-异丙基-3-甲基-6-((5-甲基-3-(三氟甲基)-1H-吡唑-4-基)甲基)噻吩并[2,3-D]嘧啶-2,4(1H,3H)-二酮
- 化合物AZD3965
- 1448671-31-5
- AZD3965,inhibit,Inhibitor,Monocarboxylate Transporter
- Thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione, 5-[[(4S)-4-hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-
- 5-{[(4S)-4-Hydroxy-4-methyl-1,2-oxazolidin-2-yl]carbonyl}-1-isopropyl-3-methyl-6-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl}thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
- AZD-3965;AZD3965;AZD 3965
- CS-2201
- (S)-5-(4-hydroxy-4-methylisoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-((5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)methyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
- 5-[[(4S)-4-Hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione