Product Details
| Product Name:
Atuveciclib |
CAS No.:
2923012-24-0 |
| Supply Ability:
10g |
Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | Atuveciclib |
| Description | Atuveciclib (BAY-1143572) is a potent and highly selective oral PTEFb/CDK9 inhibitor, demonstrating an IC50 of 13 nM in inhibiting CDK9/CycT1. |
| In vitro | Positive transcription elongation factor b (PTEFb), consisting of a CDK9-cyclin heterodimer with cyclin T1, cyclin K, cyclin T2a, or cyclin T2b, shows notable antiproliferative effects on HeLa cells (IC 50 = 920 nM) and MOLM-13 cells (IC 50 = 310 nM) when targeted with Atuveciclib (BAY-1143572) [1]. |
| In vivo | In vivo studies using the MOLM-13 xenograft mouse model show that Atuveciclib (BAY-1143572) demonstrates significant antitumor activity. Administering Atuveciclib daily at doses of 6.25 or 12.5 mg/kg leads to dose-dependent tumor suppression, with treatment-to-control (T/C) ratios of 0.64 and 0.49, respectively (p<0.001). Higher doses of 20 or 25 mg/kg result in even stronger antitumor effects, with T/C ratios dropping to 0.41 and 0.31, respectively (p<0.001), and the 25 mg/kg dose being the highest tolerated by the nude mice. Additionally, dosing Atuveciclib at 25 or 35 mg/kg on a schedule of three days on and two days off yields T/C ratios of 0.33 and 0.20, respectively (p<0.001). The compound's tolerability is confirmed by a less than 10% average reduction in body weight throughout the study period. Pharmacokinetic evaluation in rats reveals Atuveciclib has a low blood clearance rate of 1.1 L/kg per hour. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 128.5 mg/mL (331.67 mM)
|
| Keywords | Atuveciclib | BAY1143572 | BAY 1143572 |
| Inhibitors Related | Ribociclib | Ro-3306 | GSK 3 Inhibitor IX | Rafoxanide | Palbociclib monohydrochloride | CASIN | Palbociclib | GW 441756 | Sodium Oxamate | Abemaciclib | Dinaciclib | Abemaciclib methanesulfonate |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$81.00/1mg |
VIP5Y
|
TargetMol Chemicals Inc.
|
2024-11-19 |
United States