| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S83170-5mg买3赠1 |
99.03% | ￥382.00 |
4 | - | - | - | - |
|
S83170-10mg买3赠1 |
99.03% | ￥636.00 |
5 | - | - | - | - |
|
S83170-25mg买3赠1 |
99.03% | ￥1080.00 |
3 | - | - | - | - |
|
S83170-50mg买3赠1 |
99.03% | ￥2040.00 |
3 | - | - | - | - |
|
S83170-100mg |
99.03% | ￥3120.00 |
1 | - | - | - | - |
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| 产品描述： | Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib. Atuveciclib is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM | ||||||||||||||||||||
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| 靶点： | CDK9;CDK | ||||||||||||||||||||
| 体外研究： | Atuveciclib (BAY-1143572) inhibits the proliferation of 7 MLL-rearrangements positive and negative AML cell lines with a median IC50 of 385 nM (range 230-1100 nM) and induces apoptosis. Atuveciclib (BAY-1143572) has potent and highly selective PTEFb-kinase inhibitory activity in the low nanomolar range against PTEFb/CDK9 and an at least 50-fold selectivity against other CDKs. Atuveciclib (BAY-1143572) shows a favorable selectivity against a panel of non-CDK kinases. It shows broad antiproliferative activity against a panel of tumor cell lines with sub-micromolar IC50 values. The concentration-dependent inhibition of the phosphorylation of the RNA polymerase II and downstream reduction of MYC mRNA and protein levels is observed | ||||||||||||||||||||
| 体内研究： | Atuveciclib (BAY-1143572) exhibits single agent efficacy at tolerated doses in 4 out of 5 AML xenograft tumor models in mice and in 2 out of 2 AML xenograft tumor models in rats upon once daily oral administration. Partial or even complete remissions could be achieved in several models.The inhibition of MYC mRNA is also observed in blood cells of Atuveciclib (BAY-1143572)-treated rats indicating the potential clinical utility of MYC in blood cells as a pharmacodynamic marker in clinical development. The in vivo efficacy of Atuveciclib (BAY-1143572) is significantly enhanced in combination with several chemotherapeutics in different solid tumor models | ||||||||||||||||||||
| 参考文献： | 1. Scholz A, et al. BAY 1143572, a first-in-class, highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I, shows convincing anti-tumor activity in preclinical models of acute myeloid leukemia (AML). 2. Scholz A, et al. BAY 1143572: A first-in-class, highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I, inhibits MYC and shows convincing anti-tumor activity in multiple xenograft models by the induction of apoptosis | ||||||||||||||||||||
| 溶解性： | soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20°C | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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