Atuveciclib Racemate (BAY-1143572 Racemate)
(Synonyms: BAY-1143572 Racemate) 目录号 : GC34059
Atuveciclib (BAY-1143572) is potent and highly selective PTEFb/CDK9 inhibitor with IC50 values of 13 nM for CDK9/CycT and the ratio of IC50 values for CDK2/CDK9 is about 100. Outside the CDK family, It inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β respectively.
Cas No.:1414943-88-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Atuveciclib (BAY-1143572) is potent and highly selective PTEFb/CDK9 inhibitor with IC50 values of 13 nM for CDK9/CycT and the ratio of IC50 values for CDK2/CDK9 is about 100. Outside the CDK family, It inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β respectively.
BAY?1143572 is a potent and highly selective CDK9 inhibitor (IC50 CDK9/CycT1: 13?nM, ratio of IC50 values CDK2/CDK9: 100). Outside the CDK family, submicromolar inhibitory activity was only recorded against GSK3 kinase (IC50 GSK3α: 45?nM, GSK3β: 87?nM). BAY?1143572 demonstrates antiproliferative activity against HeLa cells (IC50 = 920?nM) and MOLM-13 cells (IC50 = 310?nM). It also demonstrates improved Caco-2 permeability and a decreased efflux ratio (PappA→B: 35?nm/s, ER: 6) relative to lead compound BAY‐958 (PappA→B: 22?nm/s, ER: 15)[1].
In an in?vivo pharmacokinetic study in rats, BAY?1143572 showed low blood clearance (CLb 1.1?L/h/kg). The volumes of distribution (Vss) of BAY?1143572 is 1.0?L/kg. BAY?1143572 shows significantly improved oral bioavailability of 54?%. The blood/plasma ratios is about 1. It does not show significant inhibition of cytochrome P450 activity, with IC50 values >20?μM[1]. The administration of BAY 1143572 in immunocompromized NOD/Shi-scid/IL-2Rγ null (NOG) mice xenografted with patient-derived ATL cells greatly reduced the infiltration of ATL cells into organs, such as liver and bone marrow. Decreased human soluble IL2R levels in serum were also observed, which indicated a reduction of ATL tumor burden[2].
[1] Lücking U, et al. ChemMedChem. 2017, 12(21):1776-1793. [2] Wong RWJ, et al. Molecules. 2018, 23(5). pii: E1057.
| Cas No. | 1414943-88-6 | SDF | |
| 别名 | BAY-1143572 Racemate | ||
| Canonical SMILES | N=S(CC1=CC(NC2=NC(C3=CC=C(F)C=C3OC)=NC=N2)=CC=C1)(C)=O | ||
| 分子式 | C18H18FN5O2S | 分子量 | 387.43 |
| 溶解度 | DMSO: 125 mg/mL (322.64 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5811 mL | 12.9056 mL | 25.8111 mL |
| 5 mM | 0.5162 mL | 2.5811 mL | 5.1622 mL |
| 10 mM | 0.2581 mL | 1.2906 mL | 2.5811 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。