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ATUVECICLIB RACEMATE (BAY-1143572 RACEMATE)
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- CAS号:
- 1414943-88-6
- 英文名:
- BAY-1143572.
- 英文别名:
- BAY1143572;BAY 1143572;BAY-1143572.;Atuveciclib Racemate;BAY-1143572 Racemate;Atuveciclib(BAY-1143572);ATUVECICLIB RACEMATE (BAY-1143572 RACEMATE);4-(4-fluoro-2-methoxyphenyl)-N-(3-((S-methylsulfonimidoyl)methyl)phenyl)-1,3,5-triazin-2-amine;1,3,5-Triazin-2-amine, 4-(4-fluoro-2-methoxyphenyl)-N-[3-[(S-methylsulfonimidoyl)methyl]phenyl]-;(rac)-4-(4-fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine
- 中文名:
- ATUVECICLIB RACEMATE (BAY-1143572 RACEMATE)
- 中文别名:
- 阿维西利;PTEFB/CDK9抑制剂;4-(4-氟-2-甲氧基苯基)-N-(3-((S-甲基磺酰亚胺基)甲基)苯基)-1,3,5-三嗪环-2-胺
- CBNumber:
- CB03133468
- 分子式:
- C18H18FN5O2S
- 分子量:
- 387.43
- MOL File:
- 1414943-88-6.mol
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ATUVECICLIB RACEMATE (BAY-1143572 RACEMATE)化学性质
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沸点:
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589.9±60.0 °C(Predicted)
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密度:
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1.36±0.1 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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DMSO: 125 mg/mL (322.64 mM)
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形态:
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Solid
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颜色:
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White to off-white
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ATUVECICLIB RACEMATE (BAY-1143572 RACEMATE)性质、用途与生产工艺
Atuveciclib (BAY-1143572)是一种有效的、高选择性PTEFb/CDK9抑制剂,对CDK9/CycT的IC50值为13 nM。它对CDK2的IC50是其对CDK9的约100倍。除了CDK家族成员,它还抑制GSK3激酶,对GSK3α和GSK3β的IC50值分别为45 nM和87 nM。
Target | Value |
CDK9
(Cell-free assay)
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13 nM
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GSK-3α
()
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45 nM
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GSK3β
()
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87 nM
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BAY 1143572是一种有效的、高度选择性的CDK9抑制剂,对CDK9/CycT1的IC50值为13 nM,对CDK2的IC50值是其100倍。除了CDK家族成员,在低于1 μM浓度时,BAY 1143572仅对GSK3激酶有抑制活性,对GSK3α和GSK3β的IC50值分别为45 nM和87 nM。BAY 1143572对Hela细胞和MOLM-13细胞具有抗增殖活性,IC50分别为920 nM和310 nM。相对于BAY-958,BAY 1143572的Caco-2渗透率更高,而流出比率降低。
在大鼠体内进行药代动力学研究发现,BAY 1143572的血浆清除率低(CL
b
1.1 L/h/kg),分布容积(Vss)为1.0 L/kg。其口服生物利用度为54%,血液-血浆浓度比为1。BAY 1143572对细胞色素P450活性没有显著的抑制作用,IC50>20 μM。在免疫不全的NOD/Shi-scid/IL-2Rγ。
ATUVECICLIB RACEMATE (BAY-1143572 RACEMATE)
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 | HY-12871 | Atuveciclib Racemate | | 1 mg | 750元 |
2024/08/19 | HY-12871 | ATUVECICLIB RACEMATE (BAY-1143572 RACEMATE) Atuveciclib Racemate | 1414943-88-6 | 5mg | 1800元 |
ATUVECICLIB RACEMATE (BAY-1143572 RACEMATE)
生产厂家
1414943-88-6, ATUVECICLIB RACEMATE (BAY-1143572 RACEMATE) 相关搜索:
- 药靶配体
- 抑制剂
- 细胞生物学试剂
- 4-(4-氟-2-甲氧基苯基)-N-(3-((S-甲基磺酰亚胺基)甲基)苯基)-1,3,5-三嗪环-2-胺
- 阿维西利
- PTEFB/CDK9抑制剂
- 1414943-88-6
- Atuveciclib,BAY1143572,Cyclin dependent kinase,inhibit,Inhibitor,CDK,Atuveciclib Racemate,BAY 1143572,BAY-1143572
- 1,3,5-Triazin-2-amine, 4-(4-fluoro-2-methoxyphenyl)-N-[3-[(S-methylsulfonimidoyl)methyl]phenyl]-
- BAY-1143572 Racemate
- 4-(4-fluoro-2-methoxyphenyl)-N-(3-((S-methylsulfonimidoyl)methyl)phenyl)-1,3,5-triazin-2-amine
- (rac)-4-(4-fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine
- Atuveciclib(BAY-1143572)
- Atuveciclib Racemate
- ATUVECICLIB RACEMATE (BAY-1143572 RACEMATE)
- BAY-1143572.
- BAY1143572
- BAY 1143572