Atuveciclib Racemate | BAY-1143572 Racemate | CDK Inhibitor

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Atuveciclib Racemate {[allProObj[0].p_purity_real_show]}

货号：A908334 同义名： BAY-1143572 Racemate;Atuveciclib

Atuveciclib Racemate是Atuveciclib的外消旋体。Atuveciclib（BAY 1143572）是一种选择性、可逆的 CDK9 抑制剂，IC50 为 13 nM。通过抑制 CDK9 的活性，Atuveciclib 可阻断 RNA 聚合酶 II 的磷酸化，导致短寿命抗凋亡蛋白（如 Mcl-1）的下调，从而诱导癌细胞凋亡。

Atuveciclib Racemate 化学结构
CAS号：1414943-88-6

Atuveciclib Racemate 3D分子结构
CAS号：1414943-88-6

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Atuveciclib Racemate 纯度/质量文件产品仅供科研

货号：A908334 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • ACS Appl. Nano Mater., 2025. Ambeed. [ A188026 ]; • Eur. J. Clin. Microbiol. Infect. Dis., 2025. Ambeed. [ A151161 ]; • JJC, 2025, 20(Special Issue)): 27-39. Ambeed. [ A713856 ]; • bioRxiv, 2025. Ambeed. [ A538667 , A714873 , A126729 , A126049 , A446054 ]; • Nature Communications, 2025, 16, 1871. Ambeed. [ A508148 ]; 更多 >

CDK 亚型比较

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 hydrochloride	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											SGK,ERK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinA, IC50: 70 nM CDK2/CyclinE, IC50: 35 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinA, IC50: 4 nM CDK2/CyclinE, IC50: 3 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinA, IC50: 8 nM CDK2/CyclinE, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinA, IC50: 45 nM CDK2/CyclinE, IC50: 363 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinA, IC50: 0.68μM CDK2/CyclinE, IC50: 7.5μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinA, IC50: 38 nM CDK2/CyclinE, IC50: 48 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 hydrochloride	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	99%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinA, IC50: 0.7 μM CDK2/CyclinE, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 dihydrochloride									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				99%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinA, IC50: 224 nM CDK2/CyclinE, IC50: 2.54 μM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			98%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM		99%+
(E/Z)-TG003												+++ mCLK4, IC50: 15 nM mCLK1, IC50: 200 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Atuveciclib Racemate 生物活性

描述

Atuveciclib (BAY-1143572) suppresses the growth of seven AML cell lines, both with and without MLL rearrangements, displaying a median IC50 value of 385 nM (ranging from 230 to 1100 nM) and triggers apoptosis^[1]. Atuveciclib (BAY-1143572) exhibits potent and highly selective inhibitory activity against PTEFb/CDK9 kinase within the low nanomolar range, with a selectivity that is at least 50 times greater against other CDKs. It also demonstrates favorable selectivity over a range of non-CDK kinases and broad antiproliferative effects across various tumor cell lines, achieving sub-micromolar IC50 values. A concentration-dependent decrease in the phosphorylation of RNA polymerase II, along with subsequent reductions in MYC mRNA and protein levels, has been observed^[2].

体内研究

Atuveciclib (BAY-1143572) demonstrates efficacy as a single agent in four of five AML xenograft tumor models in mice and in both tested AML xenograft tumor models in rats with daily oral doses. In several models, it leads to partial or complete remissions^[1].

The reduction of MYC mRNA levels in blood cells from rats treated with Atuveciclib (BAY-1143572) suggests the potential of using MYC in blood cells as a pharmacodynamic marker during clinical development. Additionally, the in vivo effectiveness of Atuveciclib (BAY-1143572) is significantly improved when used in conjunction with various chemotherapeutics across different solid tumor models^[2].

体外研究

Atuveciclib (BAY-1143572) exhibits potent and highly selective inhibitory activity against PTEFb/CDK9 kinase within the low nanomolar range, with a selectivity that is at least 50 times greater against other CDKs. It also demonstrates favorable selectivity over a range of non-CDK kinases and broad antiproliferative effects across various tumor cell lines, achieving sub-micromolar IC50 values. A concentration-dependent decrease in the phosphorylation of RNA polymerase II, along with subsequent reductions in MYC mRNA and protein levels, has been observed^[2].

Atuveciclib Racemate 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02345382	Leukemia	Phase 1	Completed	-	United States, Massachusetts ... 展开 >> Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02215 United States, New Jersey Hackensack University Medical Center Hackensack, New Jersey, United States, 07601 United States, New York Columbia University Medical Center New York, New York, United States, 10032 United States, South Carolina Medical University of South Carolina Charleston, South Carolina, United States, 29425 United States, Tennessee Vanderbilt University Medical Center Nashville, Tennessee, United States, 37232 Germany Universitätsklinikum der Johann Wolfgang Goethe Universität Frankfurt, Hessen, Germany, 60596 Medizinische Fakultät Carl Gustav Carus Dresden, Sachsen, Germany, 01307 收起 <<

Atuveciclib Racemate 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). [abstract]. In: Proceed

[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. [

Atuveciclib Racemate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.58mL

0.52mL

0.26mL

12.91mL

2.58mL

1.29mL

25.81mL

5.16mL

2.58mL

Atuveciclib Racemate 技术信息

CAS号	1414943-88-6
分子式	C₁₈H₁₈FN₅O₂S
分子量	387.431

别名	BAY-1143572 Racemate;Atuveciclib;BAY-1143572
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Sealed in dry,2-8°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(271.02 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

动物实验配方

Atuveciclib Racemate {[allProObj[0].p_purity_real_show]}

Atuveciclib Racemate 纯度/质量文件产品仅供科研

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Atuveciclib Racemate 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Atuveciclib Racemate 质控信息

Atuveciclib Racemate 生物活性

Atuveciclib Racemate 临床研究

Atuveciclib Racemate 参考文献

Atuveciclib Racemate 实验方案

Atuveciclib Racemate 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

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